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Geldanamycin (NSC 122750) Inhibiteur de HSP90

Name: Geldanamycin (NSC 122750)
Brand: Selleck Chemicals
SKU: S2713
Rating: 5 (36 reviews)

N° Cat.S2713

Geldanamycin est un inhibiteur naturel de HSP90 avec une K_d de 1,2 μM, qui perturbe spécifiquement l'association entre le récepteur des glucocorticoïdes (GR) et HSP. Geldanamycin atténue les ALI (lésions pulmonaires aiguës)/ARDS (syndrome de détresse respiratoire aiguë) induits par une infection virale en réduisant les réponses inflammatoires de l'hôte.

Geldanamycin (NSC 122750) Antineoplastic and Immunosuppressive Antibiotics inhibiteur Chemical Structure

Structure chimique

Poids moléculaire: 560.64

Aller à

Contrôle qualité

Lot : Pureté : 99.96%

99.96

Cibles apparentées	Akt Wnt/beta-catenin PKC HSP ROCK Microtubule Associated Integrin Bcr-Abl Actin FAK
Autre Antineoplastic and Immunosuppressive Antibiotics Inhibiteurs	Staurosporine (STS) Cyclosporin A Oligomycin A (MCH 32) Puromycin Dihydrochloride Nigericin sodium salt Honokiol Streptozotocin (STZ) Sodium Monensin (NSC 343257) Cephalomannine Pirarubicin

Culture cellulaire, traitement et concentration de travail

Lignées cellulaires	Type dessai	Concentration	Temps dincubation	Description de lactivité	PMID
A2780 cells	Proliferation assay			Compound was evaluated for antiproliferative activity against human ovarian carcinoma cell line A2780, IC50=3.4 μM	11514145
SW620 cell	Growth inhibition assay			Inhibitory concentration against human colorectal carcinoma SW620 cell lines, IC50=6.2 nM	15658879
MCF-7 cell	Growth inhibition assay			Inhibitory concentration against human breast cancer MCF-7 cell lines, IC50=6.5 nM	15658879
K562 cell	Growth inhibition assay			Inhibitory concentration against human leukemia K562 cell lines, IC50=22.1 nM	15658879
HT-29 cell	Growth inhibition assay			Inhibitory concentration against human colorectal carcinoma HT-29 cell lines, IC50=24.5 nM	15658879
SK-BR-3	Function assay	50 mg/kg		Inhibition of oncogene product p185 erbB-2 from human breast cancer cells(SK-BR-3 cells) at 50 mg/kg dose, IC50=0.07μM	7562911
SK-BR-3	Function assay			In vitro inhibition of p185 erbB-2 oncoprotein in human breast cancer SK-BR-3 cells, IC50=0.07μM	7562912
MCF-7	Function assay			Inhibition of steady-state expression of HER2 in MCF-7 breast cancer cells, IC50=0.05μM	10340605
MCF-7	Function assay			Inhibition of steady-state expression of ER in MCF-7 breast cancer cells, IC50=0.06μM	10340605
MCF-7	Function assay			Inhibition of steady-state expression of Raf-1 in MCF-7 breast cancer cells, IC50=0.2μM	10340605
SKBR-3	Function assay			Effective concentration for Her-2 degradation in SKBR-3 cells, Concentration=5μM	15713410
HEK293	Function assay			Inhibition of HSP90 expressed in HEK293 cells assessed as effect on Akt1:p27 interaction complexes by EYFP and/or YFP Venus fragment based reporter gene assay	16680159
LS174T	Cytotoxicity assay			Cytotoxicity against human LS174T cells by MTS assay, IC50=0.45μM	17034135
rat neuronal cells	Cytotoxicity assay	10 uM	24 hrs	Cytotoxicity against rat neuronal cells at 10 uM after 24 hrs	17276679
P19	Cytotoxicity assay		18 hrs	Cytotoxicity against mouse P19 cells after 18 hrs, IC50=0.1μM	17442565
MCF7	Growth inhibition assay			Growth inhibition of human MCF7 cells after days by SRB assay, GI50=35.6μM	17869098
HCT116	Growth inhibition assay			Growth inhibition of human HCT116 cells, GI50=0.021μM	18243703
DLD1	Growth inhibition assay			Growth inhibition of human DLD1 cells, GI50=0.037μM	18243703
KPL4	Growth inhibition assay			Growth inhibition of human KPL4 cells, GI50=0.059μM	18243703
A549	Growth inhibition assay			Growth inhibition of human A549 cells, GI50=0.064μM	18243703
KPL4	Function assay		40 hrs	Inhibition of Hsp90 in human KPL4 cells assessed as depletion of ErbB2 level after 40 hrs, MEC=0.11μM	18243703
KPL4	Function assay		40 hrs	Inhibition of Hsp90 in human KPL4 cells assessed as depletion of Raf-1 level after 40 hrs, MEC=0.33μM	18243703
Jurkat	Function assay	1 uM		Inhibition of to HSP90 in FADD deficient human Jurkat cells assessed as RIP protein degradation at 1 uM by Western blot	18408713
HEK293T	Function assay			Inhibition of TNF-alpha-induced NF-kappaB activation expressed in HEK293T cells by luciferase reporter gene assay	18408713
Jurkat	Function assay			Inhibition of TNF-alpha-induced NF-kappaB activation expressed in FADD deficient human Jurkat cells by luciferase reporter gene assay	18408713
SKBR3	Function assay		24 hrs	Inhibition of Hsp90-mediated HER2 degradation in human SKBR3 cells after 24 hrs by Western blot	18816111
SKBR3	Function assay		24 hrs	Inhibition of Hsp90-mediated Raf degradation in human SKBR3 cells after 24 hrs by Western blot	18816111
HuH7	Antiviral assay		3 days	Antiviral activity against Hepatitis C virus genotype 1b Con1 infected in human HuH7 cells assessed as GAPDH RNA or 18S rRNA level after 3 days by qRT-PCR analysis, EC50=0.00025μM	18936191
HuH7	Antiviral assay		3 days	Antiviral activity against Hepatitis C virus genotype 1b Con1 infected in human HuH7 cells assessed as GAPDH RNA or 18S rRNA level after 3 days selected with 40 nM HCV-796 and 800 nM boceprevir by qRT-PCR analysis, EC50=0.0012μM	18936191
SH-SY5Y	Neuroprotection assay			Neuroprotection against beta-amyloid peptide 1-42-induced toxicity in human SH-SY5Y cells assessed as lactate dehydrogenase release, EC50=0.04269μM	19138859
SH-SY5Y	Neuroprotection assay	10 nM		Neuroprotection against beta-amyloid peptide 1-42-induced toxicity in retinoic acid-differentiated human SH-SY5Y cells assessed as lactate dehydrogenase release at 10 nM	19138859
SKBR3	Cytotoxicity assay		72 hrs	Cytotoxicity against human SKBR3 cells after 72 hrs by celltiter-glo assay, IC50=0.041μM	19405528
MCF7	Cytotoxicity assay			Cytotoxicity against human MCF7 cells by SRB assay, IC50=9.6μM	19560353
SK-BR-3	Antiproliferative assay			Antiproliferative activity against human SK-BR-3 cells, IC50=0.0158μM	19896848
MCF7	Antiproliferative assay			Antiproliferative activity against human MCF7 cells, IC50=0.0161μM	19896848
A431	Antiproliferative assay		72 hrs	Antiproliferative activity against human A431 cells after 72 hrs, IC50=0.2μM	20655237
PP30	Function assay	100 uM	3 hrs	Inhibition of human HSP90alpha expressed in yeast PP30 cells co-expressing HSF-lacZ reporter assessed as induction of heat shock response at 100 uM after 3 hrs	21129982
MCF7	Function assay	0.5 uM		Inhibition of Hsp90 in human MCF7 cells assessed as Akt degradation at 0.5 uM by Western blot analysis	21273068
MCF7	Function assay	0.5 uM		Inhibition of Hsp90 in human MCF7 cells assessed as Raf degradation at 0.5 uM by Western blot analysis	21273068
MCF7	Function assay	0.5 uM		Inhibition of Hsp90 in human MCF7 cells assessed as Hsp90 degradation at 0.5 uM by Western blot analysis	21273068
MCF7	Function assay	0.5 uM		Inhibition of Hsp90 in human MCF7 cells assessed as Her2 degradation at 0.5 uM by Western blot analysis	21273068
HCT116	Antiproliferative assay		4 days	Antiproliferative activity against human HCT116 cells measured on day 4 by Cell titer-glo assay, EC50=0.03μM	21420297
HCT116	Antiproliferative assay			Antiproliferative activity against human HCT116 cells by luminescence assay, EC50=0.03μM	21605975
U87	Antiproliferative assay			Antiproliferative activity against human U87 cells by luminescence assay, EC50=0.089μM	21605975
HCT116	Antiproliferative assay			Antiproliferative activity against human HCT116 cells, IC50=0.03μM	21715165
NCI-H1975	Antiproliferative assay			Antiproliferative activity against human NCI-H1975 cells, IC50=0.036μM	21715165
U87MG	Antiproliferative assay			Antiproliferative activity against human U87MG cells, IC50=0.089μM	21715165
MCF7	Function assay	500 nM	24 hrs	Inhibition of Hsp90 in human MCF7 cells assessed as induction of Her2 degradation at 500 nM after 24 hrs by Western blot method	21861487
MCF7	Function assay	500 nM	24 hrs	Inhibition of Hsp90 in human MCF7 cells assessed as induction of Raf degradation at 500 nM after 24 hrs by Western blot method	21861487
MCF7	Function assay	500 nM	24 hrs	Inhibition of Hsp90 in human MCF7 cells assessed as induction of Akt degradation at 500 nM after 24 hrs by Western blot method	21861487
MCF7	Cytotoxicity assay		72 hrs	Cytotoxicity against human MCF7 cells at 72 hrs by MTS assay, IC50=0.053μM	22162786
HepG2	Cytotoxicity assay			Cytotoxicity against human HepG2 cells, IC50=0.37μM	22849774
SKBR3	Antiproliferative assay		72 hrs	Antiproliferative activity against estrogen receptor deficient human SKBR3 cells after 72 hrs, IC50=0.0085μM	23648180
MCF7	Antiproliferative assay		72 hrs	Antiproliferative activity against human MCF7 cells expressing estrogen receptor after 72 hrs, IC50=0.0098μM	23648180
HepG2	Cytotoxicity assay			Cytotoxicity against human HepG2 cells by MTT assay, IC50=0.3μM	23656556
SKBR3	Function assay	0.5 uM	18 hrs	Inhibition of HSP90 in human SKBR3 cells assessed as aggregation of intracellular HER2 at 0.5 uM after 18 hrs by DAPI staining-based immunofluorescence microscopic analysis	23859777
A549	Cytotoxicity assay		2 days	Cytotoxicity against human A549 cells after 2 days by AlamarBlue assay, IC50=0.15μM	23947794
CL1-5	Function assay	2 uM	16 hrs	Inhibition of HSP90 in human CL1-5 cells assessed as reduction of total Akt at 2 uM after 16 hrs by Western blotting analysis	24428777
L6	Cytotoxicity assay		72 hrs	Cytotoxicity against rat L6 cells after 72 hrs by Alamar Blue assay, IC50=6μM	24580531
Sf9	Function assay		16 hrs	Displacement of GM-BODIPY from human full length HSP90 alpha expressed in baculovirus-infected Sf9 cells after 16 hrs by fluorescence polarization assay, IC50=0.074μM	24751441
MDA-kb2	Function assay		18 hrs	Inhibition of HSP90 in human MDA-kb2 cells assessed as reduction in glucocorticoid receptor-dependent luciferase expression after 18 hrs by firefly luciferase reporter gene assay, IC50<0.01μM	24984936
MCF7	Antiproliferative assay		72 hrs	Antiproliferative activity against human MCF7 cells assessed as growth inhibition after 72 hrs by MTS/PMS assay, IC50=0.04μM	25075762
MDA-MB-231	Cytotoxicity assay		72 hrs	Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay, IC50=0.05μM	25105924
LNCAP	Cytotoxicity assay		72 hrs	Cytotoxicity against human LNCAP cells after 72 hrs by MTT assay, IC50=0.43μM	25105924
MDA-MB 231	Function assay	0.5 and 5 uM		Inhibition of HSP90 in human MDA-MB 231 cells assessed increase in HSP70 protein levels at 0.5 and 5 uM by Western blot method	25105924
HUVEC	Cytotoxicity assay		72 hrs	Cytotoxicity against HUVEC cells after 72 hrs by MTT assay, IC50=0.019μM	25277067
A431	Cytotoxicity assay		72 hrs	Cytotoxicity against human A431 cells after 72 hrs by MTT assay, IC50=0.04μM	25277067
BGC823	Cytotoxicity assay		72 hrs	Cytotoxicity against human BGC823 cells after 72 hrs by MTT assay, IC50=0.04μM	25277067
HepG2	Cytotoxicity assay		72 hrs	Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay, IC50=0.04μM	25277067
MDA-MB-231	Cytotoxicity assay		72 hrs	Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay, IC50=0.05μM	25277067
A549	Cytotoxicity assay		72 hrs	Cytotoxicity against human A549 cells after 72 hrs by MTT assay, IC50=0.097μM	25277067
HL7702	Cytotoxicity assay		72 hrs	Cytotoxicity against human HL7702 cells after 72 hrs by MTT assay, IC50=0.141μM	25277067
SW480	Cytotoxicity assay		72 hrs	Cytotoxicity against human SW480 cells after 72 hrs by MTT assay, IC50=0.31μM	25277067
HeLa	Cytotoxicity assay		72 hrs	Cytotoxicity against human HeLa cells after 72 hrs by MTT assay, IC50=0.798μM	25277067
MDA-MB 231	Function assay	0.5 uM	24 hrs	Inhibition Hsp90 in human MDA-MB 231 cells assessed as increase in HSP70 protein level at 0.5 uM incubated for 24 hrs by Western blot method	25277067
MCF7	Cytotoxicity assay		72 hrs	Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs by MTS/PMS assay, IC50=0.0427μM	25756299
MCF7	Function assay		24 hrs	Inhibition of HSP90 in human MCF7 cells assessed as pAkt degradation at 5 times IC50 after 24 hrs by Western blot analysis	25756299
MCF7	Function assay		24 hrs	Inhibition of HSP90 in human MCF7 cells assessed as Her2 degradation at 5 times IC50 after 24 hrs by Western blot analysis	25756299
MCF7	Function assay		24 hrs	Inhibition of HSP90 in human MCF7 cells assessed as Cdk6 degradation at 5 times IC50 after 24 hrs by Western blot analysis	25756299
MCF7	Function assay		24 hrs	Inhibition of HSP90 in human MCF7 cells assessed as Raf degradation at 5 times IC50 after 24 hrs by Western blot analysis	25756299
MCF7	Function assay		24 hrs	Change in Cdc37 expression in human MCF7 cells at 5 times IC50 after 24 hrs by Western blot analysis	25756299
MCF7	Function assay		24 hrs	Change in p23 expression in human MCF7 cells at 5 times IC50 after 24 hrs by Western blot analysis	25756299
MCF7	Function assay		24 hrs	Inhibition of HSP90 in human MCF7 cells assessed as induction of heat shock response-mediated HSP90 production at 5 times IC50 after 24 hrs by Western blot analysis relative to vehicle-treated control	25756299
MCF7	Function assay		24 hrs	Inhibition of HSP90 in human MCF7 cells assessed as induction of heat shock response-mediated HSP70 production at 5 times IC50 after 24 hrs by Western blot analysis relative to vehicle-treated control	25756299
MCF7	Function assay		24 hrs	Inhibition of HSP90 in human MCF7 cells assessed as induction of heat shock response-mediated HSP27 production at 5 times IC50 after 24 hrs by Western blot analysis relative to vehicle-treated control	25756299
PC12	Function assay	10 uM	3 to 16 hrs	Inhibition of D-aspartate biosynthesis in rat PC12 cells assessed as reduction of intracellular D-aspartate content at 10 uM measured at 3 to 16 hrs by O-phthalaldehyde/N-acetyl-L-cysteine derivatization technique-based HPLC analysis relative to vehicle-t	26642769
PC12	Function assay	10 uM	6 to 16 hrs	Inhibition of D-aspartate biosynthesis in rat PC12 cells assessed as reduction of total D-aspartate content at 10 uM measured at 6 to 16 hrs by O-phthalaldehyde/N-acetyl-L-cysteine derivatization technique-based HPLC analysis relative to vehicle-treated c	26642769
PC12	Function assay		24 hrs	Inhibition of D-aspartate biosynthesis in rat PC12 cells assessed as reduction of intracellular D-aspartate level up to 10 uM after 24 hrs by O-phthalaldehyde/N-acetyl-L-cysteine derivatization technique-based HPLC analysis	26642769
PC12	Function assay	up to 10 uM	24 hrs	Inhibition of D-aspartate biosynthesis in rat PC12 cells assessed as reduction of D-aspartate level in cell culture medium up to 10 uM after 24 hrs by O-phthalaldehyde/N-acetyl-L-cysteine derivatization technique-based HPLC analysis	26642769
A549	Function assay		12 to 24 hrs	Inhibition of Hsp90 in human A549 cells assessed as decrease in EGFR levels at five times IC50 value after 12 to 24 hrs by Western blot analysis	26745854
A549	Function assay		12 to 24 hrs	Inhibition of Hsp90 in human A549 cells assessed as decrease in Her2 levels at five times IC50 value after 12 to 24 hrs by Western blot analysis	26745854
A549	Function assay		12 to 24 hrs	Inhibition of Hsp90 in human A549 cells assessed as decrease in C-Raf levels at five times IC50 value after 12 to 24 hrs by Western blot analysis	26745854
SKBR3	Function assay			Inhibition of Hsp90 in human SKBR3 cells, IC50=0.07μM	26844689
BA/F3	Function assay		48 hrs	Inhibition of imatinib-resistant BCR-ABL T315I mutant (unknown origin) expressed in mouse BA/F3 cells assessed as decrease in cell viability after 48 hrs by trypan blue exclusion assay, IC50=1μM	26844689
BA/F3	Function assay		48 hrs	Inhibition of imatinib-resistant BCR-ABL E255K mutant (unknown origin) expressed in mouse BA/F3 cells assessed as decrease in cell viability after 48 hrs by trypan blue exclusion assay, IC50=1μM	26844689
BA/F3	Function assay		48 hrs	Inhibition of BCR-ABL (unknown origin) expressed in mouse BA/F3 cells assessed as decrease in cell viability after 48 hrs by trypan blue exclusion assay, IC50=5μM	26844689
MDA-MB-231	Antiproliferative assay		72 hrs	Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTS/PMS assay, Activity=0.06μM	27003516
MDA-MB-231	Antiproliferative assay		72 hrs	Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by SRB assay, IC50=0.03μM	27266997
HeLa	Antiproliferative assay		72 hrs	Antiproliferative activity against human HeLa cells after 72 hrs by SRB assay, IC50=0.06μM	27266997
SNU638	Anticancer assay		72 hrs	Anticancer activity against human SNU638 cells measured after 72 hrs by SRB assay, IC50=0.03μM	27283788
Caki1	Anticancer assay		72 hrs	Anticancer activity against human Caki1 cells measured after 72 hrs by SRB assay, IC50=0.056μM	27283788
A549	Anticancer assay		72 hrs	Anticancer activity against human A549 cells measured after 72 hrs by SRB assay, IC50=0.109μM	27283788
MDA-MB-231	Anticancer assay		72 hrs	Anticancer activity against human MDA-MB-231 cells measured after 72 hrs by SRB assay, IC50=0.11μM	27283788
HCT116	Anticancer assay		72 hrs	Anticancer activity against human HCT116 cells measured after 72 hrs by SRB assay, IC50=0.15μM	27283788
SKBR3	Antiproliferative assay		1 to 3 days	Antiproliferative activity against Her2-overexpressing human SKBR3 cells after 1 to 3 days by MTS assay, GI50=0.43μM	27783977
NCI-H1975	Antiproliferative assay		1 to 3 days	Antiproliferative activity against gefitinib-resistant human NCI-H1975 cells after 1 to 3 days by MTS assay, GI50=0.56μM	27783977
RPMI8226	Growth inhibition assay		72 hrs	Growth inhibition of human RPMI8226 cells after 72 hrs by MTS/PMS assay, GI50=0.003μM	29057043
MDA-MB-231	Antiproliferative assay		72 hrs	Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by SRB assay, IC50=0.06μM	29172085
A549	Antiproliferative assay		72 hrs	Antiproliferative activity against human A549 cells after 72 hrs by SRB assay, IC50=0.1μM	29172085
NCI-H1975	Antiproliferative assay		72 hrs	Antiproliferative activity against human NCI-H1975 cells after 72 hrs by Cell Titer 96 Aqueous One Solution cell proliferation assay, GI50=0.56μM	29202402
A549	Function assay	5 to 10 uM	24 hrs	Inhibition of HSP90alpha in human A549 cells assessed as upregulation of HSP90alpha expression at 5 to 10 uM after 24 hrs by Western blot analysis	29486954
A549	Function assay	5 to 10 uM	24 hrs	Inhibition of HSP90beta in human A549 cells assessed as upregulation of HSP90beta expression at 5 to 10 uM after 24 hrs by Western blot analysis	29486954
SKBR3	Function assay		24 hrs	Inhibition of HSP90 at N-terminus in human SKBR3 cells assessed as induction of Raf1 protein degradation incubated for 24 hrs by Western blot analysis	31591016
SKBR3	Function assay		24 hrs	Inhibition of HSP90 at N-terminus in human SKBR3 cells assessed as induction of CDK4 protein degradation incubated for 24 hrs by Western blot analysis	31591016
SKBR3	Function assay		24 hrs	Inhibition of HSP90 at N-terminus in human SKBR3 cells assessed as induction of Her2 protein degradation incubated for 24 hrs by Western blot analysis	31591016
SKBR3	Function assay		24 hrs	Inhibition of HSP90 at N-terminus in human SKBR3 cells assessed as induction of AKT protein degradation incubated for 24 hrs by Western blot analysis	31591016
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Informations chimiques, stockage et stabilité

Poids moléculaire	560.64	Formule	C₂₉H₄₀N₂O₉	Stockage (À partir de la date de réception)	3 ans-20°Cpoudre
N° CAS	30562-34-6	Télécharger le SDF		Stockage des solutions mères	1 an-80°Cen solvant 1 mois-20°Cen solvant
Synonymes	NSC 122750			Smiles	CC1CC(C(C(C=C(C(C(C=CC=C(C(=O)NC2=CC(=O)C(=C(C1)C2=O)OC)C)OC)OC(=O)N)C)C)O)OC

Solubilité

In vitro
Lot:

DMSO : 100 mg/mL (178.36 mM)
(Le DMSO contaminé par lhumidité peut réduire la solubilité. Utiliser du DMSO frais et anhydre.)

Water : Insoluble

Ethanol : Insoluble

Calculateur de molarité

Masse	Concentration	Volume	Poids moléculaire
=	×	×

Calculateur de dilution Calculateur de poids moléculaire

In vivo Lot:
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.
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.
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.
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 Validé par les laboratoires Selleck. Si vous avez besoin dajustements à cette formulation, contactez notre équipe de vente pour des tests personnalisés.	1.650mg/ml (2.94mM)	Taking the 1 mL working solution as an example, add 50 μL of 33 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validé par les laboratoires Selleck. Si vous avez besoin dajustements à cette formulation, contactez notre équipe de vente pour des tests personnalisés.	0.410mg/ml (0.73mM)	Taking the 1 mL working solution as an example, add 50 μL of 8.2 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. 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.

Calculateur de formulation in vivo (Solution claire)

Étape 1 : Entrez les informations ci-dessous (Recommandé : Un animal supplémentaire pour tenir compte des pertes pendant lexpérience)

Dosage : mg/kg Poids moyen des animaux : g Volume de dosage par animal :μL Nombre danimaux :

Étape 2 : Entrez la formulation in vivo (Ceci nest que le calculateur, pas la formulation. Veuillez nous contacter dabord sil ny a pas de formulation in vivo dans la section Solubilité.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Résultats du calcul :

Concentration de travail : mg/ml;

Méthode de préparation du liquide maître DMSO : mg médicament prédissous dans μL DMSO ( Concentration du liquide maître mg/mL, Veuillez nous contacter dabord si la concentration dépasse la solubilité du DMSO du lot de médicament. )

Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, ajouter ensuiteμL PEG300, mélanger et clarifier, ajouter ensuiteμL Tween 80, mélanger et clarifier, ajouter ensuite μL ddH₂O, mélanger et clarifier.

Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, ajouter ensuite μL Huile de maïs, mélanger et clarifier.

Remarque : 1. Assurez-vous que le liquide est clair avant dajouter le solvant suivant.
2. Assurez-vous dajouter le(s) solvant(s) dans lordre. Vous devez vous assurer que la solution obtenue lors de lajout précédent est une solution claire avant de procéder à lajout du solvant suivant. Des méthodes physiques telles que le vortex, les ultrasons ou le bain-marie peuvent être utilisées pour faciliter la dissolution.

Mécanisme daction

Targets/IC₅₀/Ki	p185 (SKBr3 cells) 70 nM HSP90 (N-terminal domain) (Cell-free assay) 0.78 μM(Kd) HSP90 (Cell-free assay) 1.2 μM(Kd)
In vitro	Geldanamycin se lie au site de liaison de l'ATP dans le domaine N-terminal des Hsp90 (résidus 1-220). Ce composé inhibe l'activité ATPase de Hsp90 de manière dose-dépendante. Il provoque un arrêt en G2 dose-dépendant et une inhibition réversible de l'entrée en phase S dans la lignée cellulaire ovarienne humaine A2780. Cette inhibition est accompagnée d'une augmentation de p53 et s'est finalement avérée dépendante de p53. Cette substance chimique provoque la polyubiquitination et la dégradation protéasomique de la protéine p185 tyrosine kinase réceptrice et présente une IC50 de 70 nM. C'est un réactif anti-tumoral typique, montrant une GI50 moyenne de 0,18 μM contre le panel de 60 lignées cellulaires tumorales humaines.
Kinase Assay	Calorimétrie par Titration Isotherme (ITC) de la Liaison des Nucléotides
Kinase Assay	Les expériences de titration sont réalisées à l'aide du système MSC. Dans chaque expérience, 16 aliquotes de 15 μL de Geldanamycin (300 μM dans 1% de DMSO) sont injectées dans 1,3 mL de protéine (31 μM dans 20 mM Tris-HCl, pH 7,5, 1 mM EDTA) à 25 °C, et les données résultantes sont ajustées après soustraction des chaleurs de dilution. Les chaleurs de dilution sont déterminées dans des expériences séparées par addition de ce composé au tampon et du tampon à la protéine. Aucune preuve de liaison du DMSO au site de liaison des nucléotides n'est observée. Les données de titration sont ajustées à l'aide d'un algorithme d'ajustement de courbe par moindres carrés non linéaire avec trois variables flottantes : stœchiométrie, constante de liaison (K_b) 1/K_d), et changement d'enthalpie d'interaction (ΔH°). Les constantes de dissociation estimées pour la liaison de ce composé à la Hsp90 de levure intacte sont de 1,22 μM, et pour la liaison au domaine N-terminal de Hsp90 sont de 0,78 μM. Aucune chaleur significative n'est observée lors de la liaison au fragment C-terminal.
In vivo	Geldanamycin (50 mg/kg) montre une inhibition de 30% des niveaux de phosphotyrosine associés à p185 chez les souris FRE/erbB-2.
Références	[1] https://pubmed.ncbi.nlm.nih.gov/9925731/ [2] https://pubmed.ncbi.nlm.nih.gov/8599864/ [3] https://pubmed.ncbi.nlm.nih.gov/8798456/ [4] https://pubmed.ncbi.nlm.nih.gov/7909494/ [5] https://pubmed.ncbi.nlm.nih.gov/7628050/ [6] https://pubmed.ncbi.nlm.nih.gov/7562911/

Informations sur lessai clinique

(données de https://clinicaltrials.gov, mis à jour le 2024-05-22)

Numéro NCT	Recrutement	Conditions	Sponsor/Collaborateurs	Date de début	Phases
NCT00003969	Completed	Unspecified Adult Solid Tumor Protocol Specific	Cancer Research UK\|National Cancer Institute (NCI)	August 1998	Phase 1

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