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Actinomycin D (Dactinomycin) Antineoplastic and Immunosuppressive Antibiotics Attivatore

Name: Actinomycin D (Dactinomycin)
Brand: Selleck Chemicals
SKU: S8964
Rating: 5 (150 reviews)

N. Cat.S8964

L'Actinomycin D (Dactinomycin, Act D, RASP-101) è un importante antibiotico polipeptidico isolato da batteri del suolo del genere Streptomyces. L'Actinomycin D (Dactinomycin) inibisce la DNA repair e blocca il cell cycle in fase G1 con IC50 di 0,42 μM e 0,4 nM, rispettivamente. L'Actinomycin D è un inibitore della sintesi di RNA e proteine in grado di sopprimere la sintesi proteica batterica. L'Actinomycin D è un attivatore dell'autophagy, induce la morte cellulare p53-indipendente e prolunga la sopravvivenza nella leucemia linfatica cronica ad alto rischio.Questo prodotto è una sostanza chimica pericolosa (tossicità acuta/infiammabile/corrosivo per la pelle). Si prega di usarlo indossando una maschera protettiva per il viso, guanti e indumenti protettivi.

Actinomycin D (Dactinomycin) Antineoplastic and Immunosuppressive Antibiotics Attivatore Chemical Structure

Struttura chimica

Peso molecolare: 1255.42

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Controllo Qualità (Quality Control)

Lotto: Purezza: 99.74%

99.74

Target correlati	HDAC PARP ATM/ATR DNA-PK WRN DNA/RNA Synthesis Topoisomerase PPAR Sirtuin Casein Kinase
Altro Antineoplastic and Immunosuppressive Antibiotics Inibitori	Staurosporine (STS) Cyclosporin A Oligomycin A (MCH 32) Puromycin Dihydrochloride Nigericin sodium salt Geldanamycin (NSC 122750) Honokiol Streptozotocin (STZ) Sodium Monensin (NSC 343257) Hygromycin B

Coltura cellulare, trattamento e concentrazione di lavoro
(Cell Culture, Treatment & Working Concentration)

Linee cellulari	Tipo di saggio	Concentrazione	Tempo di incubazione	Descrizione dell'attività	PMID
A2780	Cytotoxicity assay			Cytotoxicity against human A2780 cells, Activity = 0.0017 μM.	16562838
A549	Cytotoxicity assay		48 hrs	Cytotoxicity against human A549 cells assessed as reduction in cell viability after 48 hrs by alamar blue assay, EC50 = 0.000201 μM.	27736087
PC3	Cytotoxicity assay		48 hrs	Cytotoxicity against human PC3 cells assessed as reduction in cell viability after 48 hrs by alamar blue assay, EC50 = 0.000276 μM.	27736087
L1210	Function assay		3 hrs	Inhibition of RNA synthesis in mouse L1210 cells assessed as [3H]-uridine incorporation preincubated for 3 hrs before [3H]-uridine addition measured after 1 hr by scintillation spectrometric analysis, ED50 = 0.009 μM.	330857
L1210	Function assay		3 hrs	Inhibition of DNA synthesis in mouse L1210 cells assessed as [3H]-thymidine incorporation preincubated for 3 hrs before [3H]-thymidine addition measured after 1 hr by scintillation spectrometric analysis, ED50 = 0.4 μM.	330857
L1210	Function assay			Inhibition of RNA synthesis in mouse L1210 cells by [3H]-uridine incorporation assay, ED50 = 0.015 μM.	573799
L1210	Function assay			Inhibition of DNA synthesis in mouse L1210 cells by [3H]-thymidine incorporation assay, ED50 = 0.6 μM.	573799
P388	Function assay			Concentration required for 50% inhibition of incorporation of labeled uridine by P388 cells for the synthesis of RNA (in vitro), ED50 = 0.046 μM.	6169834
P388	Function assay			Concentration required for 50% inhibition of incorporation of labeled thymidine by p388 cells for synthesis of DNA (in vitro), ED50 = 0.996 μM.	6169834
HMO2	Cytotoxicity assay		48 hrs	Cytotoxicity against human HMO2 cells after 48 hrs by sulforhodamine assay, GI50 = 0.3 μM.	10757717
MCF7	Cytotoxicity assay		48 hrs	Cytotoxicity against human MCF7 cells after 48 hrs by sulforhodamine assay, GI50 = 0.5 μM.	10757717
HepG2	Cytotoxicity assay		48 hrs	Cytotoxicity against human HepG2 cells after 48 hrs by sulforhodamine assay, GI50 = 1 μM.	10757717
B104-1-1	Growth inhibitory assay			Growth inhibitory activity was tested against B104-1-1 cells, GI50 = 0.0007 μM.	10888331
Hep G2	Cytotoxicity assay			Cytotoxicity against human Hep G2 cells, GI50 = 0.0012 μM.	16933866
HM02	Cytotoxicity assay			Cytotoxicity against human HM02 cells, GI50 = 0.0016 μM.	16933866
P388	Antiproliferative assay		48 hrs	Antiproliferative activity against mouse P388 cells after 48 hrs by MTT assay, IC50 = 0.0002 μM.	2778449
HT-29	Antiproliferative assay		96 hrs	Antiproliferative activity against human HT-29 cells after 96 hrs by MTT assay, IC50 = 0.223 μM.	2778449
L1210	Function assay			Inhibition of synthesis of [5-3H]-uridine into RNA in L1210 cells., IC50 = 0.019 μM.	3397991
L1210	Function assay			Inhibition of synthesis of [methyl-14C] thymidine into DNA, in L1210 cells., IC50 = 0.38 μM.	3397991
Jurkat T	Function assay			Inhibitory concentration against Human Jurkat T cells, IC50 = 0.0045 μM.	10212121
B104-1-1	Function assay			In vitro binding assay of Shc-derived phosphopeptide to Growth factor receptor bound protein 2 SH2 in B104-1-1 cells was determined, IC50 = 5 μM.	10888331
Jurkat T	Function assay		48 hrs	Inhibitory concentration was evaluated on human Jurkat T-cells after their exposure for 48 hours, IC50 = 0.0045 μM.	11052798
C8166	Antitumor assay			Antitumor activity against CD+ human acute T-lymphoblastic leukemia C8166 cells, IC50 = 0.0008 μM.	12431048
CCRF-CEM	Antitumor assay			Antitumor activity against human acute T-lymphoblastic leukemia CCRF-CEM cells, IC50 = 0.001 μM.	12431048
CD4+T	Antitumor assay			Antitumor activity against human CD4+T cells expressing the TAT gene of HTLV-1 MT-4 cells, IC50 = 0.001 μM.	12431048
MOLT-4	Antitumor assay			Antitumor activity against human acute T-lymphoblastic leukemia MOLT-4 cells, IC50 = 0.001 μM.	12431048
G-361	Antitumor assay			Antitumor activity against human skin melanoma G-361 cells, IC50 = 0.001 μM.	12431048
MT-4	Antitumor assay			Antitumor activity against CD+ human acute T-lymphoblastic leukemia MT-4 cells, IC50 = 0.001 μM.	12431048
CCRF-SB	Antitumor assay			Antitumor activity against human acute B-lymphoblastic leukemia CCRF-SB cells, IC50 = 0.002 μM.	12431048
SKMEK-28	Antitumor assay			Antitumor activity against human skin melanoma SKMEK-28 cells, IC50 = 0.002 μM.	12431048
Raji	Antitumor assay			Antitumor activity against human Burkitt lym phoma Raji cells, IC50 = 0.002 μM.	12431048
5637	Antitumor assay			Antitumor activity against human bladder carcinoma 5637 cells, IC50 = 0.003 μM.	12431048
Wil2-NS	Antitumor assay			Anti tumor activity against human splenic B-lympho blastoid Wil2-NS cells, IC50 = 0.003 μM.	12431048
Hep-2	Antitumor assay			Antitumor activity against larynx carcinoma Hep-2 cells, IC50 = 0.004 μM.	12431048
SK-MES-1	Antitumor assay			Antitumor activity against human lung squamous carcinoma SK-MES-1 cells, IC50 = 0.004 μM.	12431048
ACHN	Antitumor assay			Antitumor activity against human renal adenocarcinoma ACHN cells, IC50 = 0.005 μM.	12431048
KB	Function assay			Compound concentration required to reduce the cell proliferation of Wild type and Drug- resistant human nasopharyngeal carcinoma KB cells by 50%, IC50 = 0.005 μM.	12431048
HT-29	Antitumor assay			Antitumor activity against human colon adenocarcinoma HT-29 cells, IC50 = 0.006 μM.	12431048
MCF-7	Antitumor assay			Antitumor activity against human breast adenocarcinoma MCF-7 cells, IC50 = 0.006 μM.	12431048
CRL7065	Antitumor assay			Antitumor activity against human foreskin fibroblasts CRL7065 cells, IC50 = 0.007 μM.	12431048
DU145	Antitumor assay			Antitumor activity against human prostate carcinoma DU145 cells, IC50 = 0.008 μM.	12431048
Hela	Antitumor assay			Antitumor activity against cervix carcinoma Hela cells cells, IC50 = 0.008 μM.	12431048
HepG2	Antitumor assay			Antitumor activity against human hepatocellular carcinoma HepG2 cells, IC50 = 0.01 μM.	12431048
C8166	Antitumor assay			Antitumor activity against CD4+ human acute T-lymphoblastic C8166 leukemia cells., IC50 = 0.00008 μM.	12431049
MT-4	Antitumor assay			Antitumor activity against CD4+ human acute T-lymphoblastic MT-4 leukemia cells., IC50 = 0.0009 μM.	12431049
G361	Antitumor assay			Antitumor activity against human skin melanoma G361 cells., IC50 = 0.001 μM.	12431049
MOLT-4	Antitumor assay			Antitumor activity against human acute T-lymphoblastic MOLT-4 leukemia cells., IC50 = 0.001 μM.	12431049
CCRF-SB	Antitumor assay			Antitumor activity against human acute B-lymphoblastic CCRF-SB leukemia cells., IC50 = 0.001 μM.	12431049
Raji	Antitumor assay			Antitumor activity against human Burkitt lymphoma Raji cells., IC50 = 0.002 μM.	12431049
5637	Antitumor assay			Antitumor activity against human bladder carcinoma 5637 cells., IC50 = 0.003 μM.	12431049
CCRF-CEM	Antitumor assay			Antitumor activity against human acute T-lymphoblastic CCRF-CEM leukemia cells., IC50 = 0.003 μM.	12431049
Wil-NS	Antitumor assay			Antitumor activity against human splenic B-lymphoblastoid Wil-NS cells., IC50 = 0.003 μM.	12431049
Hep-2	Antitumor assay			Antitumor activity against Hep-2 larynx carcinoma cells., IC50 = 0.004 μM.	12431049
ACHN	Antitumor assay			Antitumor activity against human renal adenocarcinoma ACHN cells., IC50 = 0.005 μM.	12431049
MCF-7	Antitumor assay			Antitumor activity against human breast adenocarcinoma MCF-7 cells., IC50 = 0.006 μM.	12431049
HT-29	Antitumor assay			Antitumor activity against human colon adenocarcinoma HT-29 cells., IC50 = 0.006 μM.	12431049
HepG-2	Antitumor assay			Antitumor activity against human hepatocellular carcinoma HepG-2 cells., IC50 = 0.01 μM.	12431049
HeLa	Antitumor assay			Antitumor activity against HeLa cervical carcinoma cells., IC50 = 0.04 μM.	12431049
CCRF-CEM	Cytotoxicity assay			Cytotoxicity in human leukemic CCRF-CEM cells., IC50 = 1.6 μM.	14667232
A2780	Cytotoxicity assay			Cytotoxicity against human A2780 cells, IC50 = 0.0008 μM.	15844934
A2780	Cytotoxicity assay			Cytotoxicity against human A2780 cells, IC50 = 0.0008 μM.	16180816
HeLa	Cytotoxicity assay		48 hrs	Cytotoxicity against human HeLa cells in log-phase after 48 hrs by MTT assay, IC50 = 0.001 μM.	16309323
Vero	Cytotoxicity assay		48 hrs	Cytotoxicity against african green monkey Vero cells in log-phase after 48 hrs by MTT assay, IC50 = 0.001 μM.	16309323
Hep2	Cytotoxicity assay		48 hrs	Cytotoxicity against human Hep2 cells in log-phase after 48 hrs by MTT assay, IC50 = 0.006 μM.	16309323
HeLa	Cytotoxicity assay		48 hrs	Cytotoxicity against human HeLa cells in lag-phase after 48 hrs by MTT assay, IC50 = 0.011 μM.	16309323
Vero	Cytotoxicity assay		48 hrs	Cytotoxicity against african green monkey Vero cells in lag-phase after 48 hrs by MTT assay, IC50 = 0.071 μM.	16309323
Hep2	Cytotoxicity assay		48 hrs	Cytotoxicity against human Hep2 cells in lag-phase after 48 hrs by MTT assay, IC50 = 0.191 μM.	16309323
MOLT3	Cytotoxicity assay			Cytotoxicity against MOLT3 Leukemia cells by MTS assay, IC50 = 1 μM.	16420056
U937	Cytotoxicity assay			Cytotoxicity against U937 Lymphoma cells by MTS assay, IC50 = 1 μM.	16420056
Vero	Cytotoxicity assay			Cytotoxicity against normal vero kidney cells by MTS assay, IC50 = 11 μM.	16420056
Wil2-NS	Antiproliferative assay			Antiproliferative activity against human Wil2-NS cells by MTT assay, IC50 = 0.003 μM.	16913700
HeLa	Antiproliferative assay			Antiproliferative activity against human HeLa cells by MTT assay, IC50 = 0.04 μM.	16913700
CCRF-CEM	Cytotoxicity assay		72 hrs	Cytotoxicity against human CCRF-CEM cells after 72 hrs, IC50 = 0.0016 μM.	18329887
HeLa	Antiproliferative assay		48 hrs	Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay, IC50 = 0.0004 μM.	18461997
HT29	Antiproliferative assay		48 hrs	Antiproliferative activity against human HT29 cells after 48 hrs by MTT assay, IC50 = 0.0029 μM.	18461997
U2OS	Antiproliferative assay		48 hrs	Antiproliferative activity against human U2OS cells after 48 hrs by MTT assay, IC50 = 0.0032 μM.	18461997
HeLa	Function assay		2 hrs	Inhibition of transcriptional activity in human HeLa cells assessed as [3H]uridine utilization after 2 hrs by scintillation counting, IC50 = 0.2624 μM.	20118940
HeLa	Function assay		2 hrs	Inhibition of protein synthesis in human HeLa cells assessed as [35S]cysteine/methionine utilization after 2 hrs by scintillation spectroscopy, IC50 = 0.5197 μM.	20118940
NCI-H460	Cytotoxicity assay		72 hrs	Cytotoxicity against human NCI-H460 cells after 72 hrs by MTS reduction assay, IC50 = 0.008 μM.	20704331
SF268	Cytotoxicity assay		72 hrs	Cytotoxicity against human SF268 cells after 72 hrs by MTS reduction assay, IC50 = 0.016 μM.	20704331
MCF7	Cytotoxicity assay		72 hrs	Cytotoxicity against human MCF7 cells after 72 hrs by MTS reduction assay, IC50 = 0.103 μM.	20704331
Vero	Cytotoxicity assay		20 hrs	Cytotoxicity against african green monkey Vero cells after 20 hrs by MTS assay, IC50 = 11 μM.	21093966
HeLa	Cytotoxicity assay		48 hrs	Cytotoxicity against human HeLa cells assessed as cell viability after 48 hrs by MTT assay, IC50 = 0.0011 μM.	22705001
A549	Cytotoxicity assay		48 hrs	Cytotoxicity against human A549 cells assessed as cell viability after 48 hrs by MTT assay, IC50 = 0.0072 μM.	22705001
MCF7	Cytotoxicity assay		48 hrs	Cytotoxicity against human MCF7 cells assessed as cell viability after 48 hrs by MTT assay, IC50 = 0.024 μM.	22705001
Vero	Cytotoxicity assay		48 hrs	Cytotoxicity against african green monkey Vero cells assessed as cell viability after 48 hrs by MTT assay, IC50 = 0.071 μM.	22705001
HeLa	Cytotoxicity assay		48 hrs	Cytotoxicity against human HeLa cells in lag phase of growth after 48 hrs, IC50 = 0.0011 μM.	24709561
HeLa	Cytotoxicity assay		48 hrs	Cytotoxicity against human HeLa cells in log phase of growth after 48 hrs, IC50 = 0.0016 μM.	24709561
Hep2	Cytotoxicity assay		48 hrs	Cytotoxicity against human Hep2 cells in log phase of growth after 48 hrs, IC50 = 0.0062 μM.	24709561
Vero	Cytotoxicity assay		48 hrs	Cytotoxicity against African green monkey Vero cells in log phase of growth after 48 hrs, IC50 = 0.01 μM.	24709561
Vero	Cytotoxicity assay		48 hrs	Cytotoxicity against African green monkey Vero cells in lag phase of growth after 48 hrs, IC50 = 0.072 μM.	24709561
Hep2	Cytotoxicity assay		48 hrs	Cytotoxicity against human Hep2 cells in lag phase of growth after 48 hrs, IC50 = 0.17 μM.	24709561
HEK293	Function assay		30 mins	Inhibition of human DDR2 expressed in HEK293 cells assessed as reduction in collagen-1-induced DDR2 tyrosine phosphorylation pre-incubated for 30 mins by immunoblotting method, IC50 = 9 μM.	25569119
HeLa	Cytotoxicity assay		48 hrs	Cytotoxicity against human HeLa cells assessed as reduction in cell viability using compound addition to cell culture cells in lag phase of growth and incubated for 48 hrs by MTT assay, IC50 = 0.0011 μM.	28923386
A549	Cytotoxicity assay		48 hrs	Cytotoxicity against human A549 cells assessed as reduction in cell viability using compound addition to cell culture cells in lag phase of growth and incubated for 48 hrs by MTT assay, IC50 = 0.0072 μM.	28923386
Vero	Cytotoxicity assay		48 hrs	Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability using compound addition to cell culture cells in log phase of growth and incubated for 48 hrs by MTT assay, IC50 = 0.011 μM.	28923386
MCF7	Cytotoxicity assay		48 hrs	Cytotoxicity against human MCF7 cells assessed as reduction in cell viability using compound addition to cell culture cells in lag phase of growth and incubated for 48 hrs by MTT assay, IC50 = 0.024 μM.	28923386
Vero	Cytotoxicity assay		48 hrs	Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability using compound addition to cell culture cells in lag phase of growth and incubated for 48 hrs by MTT assay, IC50 = 0.071 μM.	28923386
B16	Growth inhibition assay			In vitro 50% Growth inhibition of sensitive B16 cells., ID50 = 0.003 μM.	3397991
L1210	Growth inhibition assay			50% Inhibition of growth of L1210 cells in culture., ID50 = 0.0601 μM.	3397991
P388/ADR	Growth inhibition assay			In vitro 50% Growth inhibition of actinomycin resistant P388/ADR cells, ID50 = 2.5 μM.	3397991
HeLa	Apoptosis assay			Induction of apoptosis in human HeLa cells assessed as DNA fragmentation by agarose gel electrophoresis	22705001
NCI-H157	Apoptosis assay	10 uM	5 hrs	Induction of apoptosis in human NCI-H157 cells assessed as live cell level at 10 uM incubated for 5 hrs in serum-free medium by annexin V/propidium iodide staining by flow cytometry	22863528
HeLa	Cytotoxicity assay	1 uM	18 hrs	Cytotoxicity against human HeLa cells assessed as reduction in cell viability at 1 uM after 18 hrs by inverse MTT assay	25028062
TC32	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells	29435139
U-2 OS	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells	29435139
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
DAOY	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells	29435139
Saos-2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells	29435139
BT-37	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells	29435139
RD	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	29435139
SK-N-SH	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells	29435139
BT-12	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells	29435139
MG 63 (6-TG R)	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells	29435139
OHS-50	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	29435139
BT-12	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells	29435139
LAN-5	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells	29435139
DAOY	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells	29435139
SK-N-SH	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells	29435139
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells)	29435139
BT-37	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells	29435139
MG 63 (6-TG R)	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells	29435139
U-2 OS	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells	29435139
OHS-50	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells	29435139
SK-N-SH	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for SK-N-SH cells	29435139
Rh41	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells	29435139
Daoy	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for Daoy cells	29435139
TC32	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for TC32 cells	29435139
MG 63 (6-TG R)	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for MG 63 (6-TG R) cells	29435139
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells	29435139
SJ-GBM2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells	29435139
TC32	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells	29435139
SJ-GBM2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for SJ-GBM2 cells	29435139
RD	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for RD cells	29435139
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Informazioni chimiche, conservazione e stabilità (Chemical Information, Storage & Stability)

Peso molecolare	1255.42	Formula	C₆₂H₈₆N₁₂O₁₆	Conservazione (Dalla data di ricezione)	3 years -20°C(in the dark) powder
N. CAS	50-76-0	--		Conservazione delle soluzioni stock	1 anno-80°Cin solvente 1 mese-20°Cin solvente

Solubilità (Solubility)

In vitro
Lotto:

DMSO : 100 mg/mL (79.65 mM)
(Il DMSO contaminato da umidità può ridurre la solubilità. Utilizzare DMSO fresco e anidro.)

Water : Insoluble

Ethanol : Insoluble

Calcolatore di Molarità

Massa	Concentrazione	Volume	Peso molecolare
=	×	×

Calcolatore di Diluizione Calcolatore del Peso Molecolare

In vivo Lotto:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validato dai laboratori Selleck. Se necessiti di modifiche a questa formulazione, contatta il nostro team di vendita per test personalizzati.	3.750mg/ml (2.99mM)	Taking the 1 mL working solution as an example, add 50 μL 75 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

Calcolatore di formulazione in vivo (Soluzione chiara)

Passo 1: Inserire le informazioni di seguito (Consigliato: Un animale aggiuntivo per tenere conto della perdita durante l'esperimento)

Dosaggio: mg/kg Peso medio degli animali: g Volume di dosaggio per animale:μL Numero di animali:

Passo 2: Inserire la formulazione in vivo (Questo è solo il calcolatore, non la formulazione. Contattateci prima se non c'è una formulazione in vivo nella sezione Solubilità.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Risultati del calcolo:

Concentrazione di lavoro: mg/ml;

Metodo per preparare il liquido master di DMSO: mg farmaco predissolto in μL DMSO ( Concentrazione del liquido master mg/mL, Vi preghiamo di contattarci prima se la concentrazione supera la solubilità del DMSO del lotto del farmaco. )

Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungereμL PEG300, mescolare e chiarire, quindi aggiungereμL Tween 80, mescolare e chiarire, quindi aggiungere μL ddH₂O, mescolare e chiarire.

Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungere μL Olio di mais, mescolare e chiarire.

Nota: 1. Si prega di assicurarsi che il liquido sia limpido prima di aggiungere il solvente successivo.
2. Assicurarsi di aggiungere il/i solvente/i in ordine. È necessario assicurarsi che la soluzione ottenuta, nell'aggiunta precedente, sia una soluzione limpida prima di procedere all'aggiunta del solvente successivo. Metodi fisici come il vortex, gli ultrasuoni o il bagno d'acqua calda possono essere utilizzati per facilitare la dissoluzione.

Meccanismo d'azione (Mechanism of Action)

Targets/IC₅₀/Ki	autophagy cell cycle (Cell-based assay) 0.4 nM DNA repair (Cell-free assay) 0.42 μM
In vitro	L'Actinomycin D (Dactinomycin) riduce marcatamente la proliferazione delle SMC tramite l'inibizione dell'incorporazione di BrdU a 80 nM. Questo è ulteriormente supportato dall'arresto in fase G1 utilizzando un'analisi citofluorimetrica. I livelli di espressione proteica dell'antigene nucleare delle cellule proliferanti (PCNA), della chinasi di adesione focale (FAK) e di Raf sono tutti soppressi da questo composto. Le chinasi regolate da segnali extracellulari (Erk) coinvolte nell'arresto del ciclo cellulare risultano aumentate da esso.
In vivo	L'Actinomycin D (Dactinomycin) colpisce le proteine di sopravvivenza TOSO, BCL2 e MCL1 ed è attiva in due diversi modelli murini caratterizzati da un recettore delle cellule B non mutato o da una funzione p53 inattiva, entrambi noti fattori prognostici negativi nella LLC.
Riferimenti	[1] https://pubmed.ncbi.nlm.nih.gov/15959627/ [2] https://pubmed.ncbi.nlm.nih.gov/9450493/ [3] https://pubmed.ncbi.nlm.nih.gov/22743622/

Applicazioni (Applications)

Metodi	Biomarcatori	PMID
Western blot	L11 / L23 / p53 / MDM2 / p21 / Tubulin L23 / p53 / MDM2 / p21 / Tubulin NAT10 / p53 / Ac-p53-K120 / Mdm2 / p21 / β-actin AIF / Histone H3 / GAPDH PAR	15314173
Growth inhibition assay	Cell viability Cell Number Cell viability	26728659
SYTOX Green plate reader assay	DNA release	29736268
Immunofluorescence	DNA GFP-NAT10 NAT10 / p53 Tom20 / AIF PAR PAR	29736268

Informazioni sullo studio clinico (Clinical Trial Information)

(dati da https://clinicaltrials.gov, aggiornato il 2024-05-22)

Numero NCT	Reclutamento	Condizioni	Sponsor/Collaboratori	Data di inizio	Fasi
NCT06252285	Recruiting	RSV Immunisation	Sanofi Pasteur a Sanofi Company\|Sanofi	February 6 2024	Phase 3
NCT05858723	Not yet recruiting	Allergic Contact Dermatitis	National Allergy Research Center Denmark	August 2023	Not Applicable

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