Name: Cladribine
Brand: Selleck Chemicals
SKU: S1199
Rating: 5 (25 reviews)

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Controllo Qualità

Lotto: Purezza: 99.99%

99.99

Target correlati	Adrenergic Receptor AChR 5-HT Receptor COX Calcium Channel Histamine Receptor Dopamine Receptor GABA Receptor TRP Channel Cholinesterase (ChE)
Altro Adenosine Deaminase Inibitori	Hibifolin

Coltura cellulare, trattamento e concentrazione di lavoro

Linee cellulari	Tipo di saggio	Tempo di incubazione	Descrizione dellattività	PMID
CCRF-CEM cell lines	Cytotoxicity assay		Compound was tested for cytotoxicity against CCRF-CEM cell lines, IC50=0.003 μM	1732556
HEp-2 cell lines	Cytotoxicity assay		Compound was tested for cytotoxicity against HEp-2 cell lines, IC50=0.03 μM	1732556
L1210 cell lines	Cytotoxicity assay		Compound was tested for cytotoxicity against L1210 cell lines, IC50=0.07 Μm	1732556
CCRF-CEM cells	Cytotoxicity assay	72 h	Cytotoxicity against human CCRF-CEM cells after 72 hrs by MTT assay, IC50=0.0005 μM	21840722
human Raji cells	Cytotoxicity assay	72 h	Cytotoxicity against human Raji cells after 72 hrs by MTT assay, IC50=0.009 μM	21840722
human HuH7 cells	Cytotoxicity assay	72 h	Cytotoxicity against human HuH7 cells after 72 hrs by SRB assay, IC50=1.8 μM	25462277
human T47D cells	Cytotoxicity assay	72 h	Cytotoxicity against human T47D cells after 72 hrs by SRB assay, IC50=0.7 μM	25462277
human HCT116 cells	Cytotoxicity assay	72 h	Cytotoxicity against human HCT116 cells after 72 hrs by SRB assay, IC50=0.3 μM	25462277
human K562 cells	Proliferation assay	48 h	Antiproliferative activity against human K562 cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50=10 μM	25960323
human SKHEP1 cells	Proliferation assay	48 h	Antiproliferative activity against human SKHEP1 cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50=4 μM	25960323
human MOLT3 cells	Proliferation assay	48 h	Antiproliferative activity against human MOLT3 cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50=2.3 μM	25960323
human KG1 cells	Proliferation assay	48 h	Antiproliferative activity against human KG1 cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50=0.2 μM	25960323
human RPMI8226 cells	Proliferation assay	48 h	Antiproliferative activity against human RPMI8226 cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50=6 μM	25960323
human MCF7 cells	Proliferation assay	48 h	Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50=45 μM	25960323
human SK-UT-1B cells	Proliferation assay	48 h	Antiproliferative activity against human SK-UT-1B cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50=1 μM	25960323
L1210 cell lines	Function assay		In vitro inhibitory effect was tested for cytostatic activity on the growth of murine leukemic L1210 cell lines, ID50=0.03 μM	2995666
P388 leukemic cell lines	Function assay		In vitro inhibitory effect was tested for cytostatic activity on the growth of lymphoid neoplasm P388 leukemic cell lines, ID50=0.03 μM	2995666
BV173	Cytotoxicity assay	3 days	Cytotoxicity against human BV173 cells after 3 days by MTT assay, IC50=0.0008μM	21711054
BT549	Cytotoxicity assay	3 days	Cytotoxicity against human BT549 cells after 3 days by MTT assay, IC50=0.123μM	21711054
CT26	Cytotoxicity assay	3 days	Cytotoxicity against mouse CT26 cells after 3 days by MTT assay, IC50=0.131μM	21711054
MES-SA	Cytotoxicity assay	3 days	Cytotoxicity against human MES-SA cells after 3 days by MTT assay, IC50=0.165μM	21711054
K562	Cytotoxicity assay	3 days	Cytotoxicity against human paclitaxel resistant K562 cells after 3 days by MTT assay, IC50=0.17μM	21711054
P388D1	Cytotoxicity assay	3 days	Cytotoxicity against mouse P388D1 cells after 3 days by MTT assay, IC50=0.285μM	21711054
CEM-DNR-bulk	Cytotoxicity assay	3 days	Cytotoxicity against human CEM-DNR-bulk cells after 3 days by MTT assay, IC50=0.352μM	21711054
L1210	Cytotoxicity assay	3 days	Cytotoxicity against mouse L1210 cells after 3 days by MTT assay, IC50=0.393μM	21711054
EL4	Cytotoxicity assay	3 days	Cytotoxicity against mouse EL4 cells after 3 days by MTT assay, IC50=0.848μM	21711054
MCF7	Cytotoxicity assay	3 days	Cytotoxicity against human MCF7 cells after 3 days by MTT assay, IC50=2.35μM	21711054
K562	Cytotoxicity assay	3 days	Cytotoxicity against human K562 cells after 3 days by MTT assay, IC50=7.69μM	21711054
PC3	Cytotoxicity assay	3 days	Cytotoxicity against human PC3 cells after 3 days by MTT assay, IC50=8.28μM	21711054
C6	Cytotoxicity assay	3 days	Cytotoxicity against rat C6 cells after 3 days by MTT assay, IC50=9.07μM	21711054
HPAC	Cytotoxicity assay	3 days	Cytotoxicity against human HPAC cells after 3 days by MTT assay, IC50=9.32μM	21711054
HCT116	Cytotoxicity assay	3 days	Cytotoxicity against human HCT116 cells after 3 days by MTT assay, IC50=9.43μM	21711054
HT-29	Cytotoxicity assay	3 days	Cytotoxicity against human HT-29 cells after 3 days by MTT assay, IC50=9.44μM	21711054
HCT116	Cytotoxicity assay	72 hrs	Cytotoxicity against human HCT116 cells assessed as growth inhibition after 72 hrs by SRB assay, IC50=0.3μM	28219046
HuH7	Cytotoxicity assay	72 hrs	Cytotoxicity against human HuH7 cells assessed as growth inhibition after 72 hrs by SRB assay, IC50=1.8μM	28219046
MCF7	Cytotoxicity assay	72 hrs	Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs by SRB assay, IC50=2μM	28219046
TC32	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells	29435139
SJ-GBM2	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	29435139
A673	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 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
BT-37	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells	29435139
NB1643	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	29435139
LAN-5	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 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
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
NB1643	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells	29435139
A673	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 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
BT-37	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells	29435139
TC32	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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: Confirmatory screen for MG 63 (6-TG R) cells	29435139
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Informazioni chimiche, conservazione e stabilità

Peso molecolare	285.69	Formula	C₁₀H₁₂ClN₅O₃	Conservazione (Dalla data di ricezione)	3 anni-20°Cpolvere
N. CAS	4291-63-8	Scarica SDF		Conservazione delle soluzioni stock	1 anno-80°Cin solvente 1 mese-20°Cin solvente
Sinonimi	2-CdA,2-Chloro-2′-deoxyadenosine,CldAdo,Jk 6251,NSC 105014,RWJ 26251			Smiles	C1C(C(OC1N2C=NC3=C(N=C(N=C32)Cl)N)CO)O

Solubilità

In vitro
Lotto:

DMSO : 57 mg/mL (199.51 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 30%PEG300 2 1%Tween80 3 64%ddH2O Validato dai laboratori Selleck. Se necessiti di modifiche a questa formulazione, contatta il nostro team di vendita per test personalizzati.	10.000mg/ml (35.00mM)	Taking the 1 mL working solution as an example, add 50 μL of 200 mg/ml clarified DMSO stock solution to 300 μL of PEG300, mix evenly to clarify it; add 10 μL of Tween80 to the above system, mix evenly to clarify it; then continue to add 640 μL of 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.
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.

Calcolatore di formulazione in vivo (Soluzione chiara)

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

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 cè 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, nellaggiunta precedente, sia una soluzione limpida prima di procedere allaggiunta del solvente successivo. Metodi fisici come il vortex, gli ultrasuoni o il bagno dacqua calda possono essere utilizzati per facilitare la dissoluzione.

Meccanismo dazione

Caratteristiche	Cladribine is primarily active in lymphoid tissues.
Targets/IC₅₀/Ki	Adenosine deaminase (MM1.S cells) 0.18 μM Adenosine deaminase (RPMI8226 cells) 0.75 μM Adenosine deaminase (U266 cells) 2.43 μM
In vitro	Cladribine esercita una notevole attività nella leucemia a cellule capellute (HCL), un disturbo linfoproliferativo cronico delle cellule B, producendo remissioni complete prolungate. Questo composto induce l'accumulo di rotture del filamento di DNA e successivamente attiva il soppressore tumorale p53 nei linfociti. Può modulare l'attività di STAT3 nelle cellule MM. Questa sostanza chimica inibisce la proliferazione/sopravvivenza delle cellule U266, RPMI8226 e MM1.S in modo dose-dipendente. Mentre U266 è la linea cellulare meno sensibile, MM1.S è la più sensibile alla cladribina. Il trattamento con questo composto aumenta gradualmente la percentuale di cellule in fase G1 del ciclo cellulare e riduce la percentuale di cellule in fase S. Sembra aumentare la fase G2-M nelle cellule U266 dopo un trattamento di 24 ore. Un aumento dose-dipendente dell'apoptosi indotta da questo agente è osservato sia nelle cellule RPMI8226 che in quelle MM1.S. Il trattamento con esso a 0,2 μM induce drammaticamente l'attivazione della caspasi-3, -8 e -9 e la scissione di PARP in modo tempo-dipendente in MM1.S. Questo composto diminuisce significativamente i livelli di fosfo-STAT3 (P-STAT3) in modo dose-dipendente, ma non ha alcun effetto sui livelli totali di proteina STAT3. Possiede un potenziale induttore di apoptosi concentrazione-dipendente nelle cellule HSB2. Questa sostanza chimica inibisce la crescita dei mastociti primari (MC) e della linea MC HMC-1 in modo dose-dipendente, con valori di IC50 inferiori registrati nelle cellule HMC-1.2 che ospitano KIT D816V rispetto alle cellule HMC-1.1 prive di KIT D816V. Diminuisce la capacità migratoria dei monociti CD14⁺, così come dei linfociti T CD4⁺ e CD8⁺.
In vivo	Cladribine (0,7-3,5 mM) e/o diltiazem (2,4 mM) vengono iniettati per via intraperitoneale in pesci zebra adulti e i lisati di globuli rossi (RBC) vengono analizzati mediante HPLC per i livelli di nucleotidi purinici (ad esempio ATP), potenziali biomarcatori della salute cardiovascolare. Il diltiazem ha aumentato le concentrazioni di ATP nei globuli rossi, che sono inibite dalla co-iniezione di questo composto. Le concentrazioni plasmatiche di questa sostanza chimica diminuiscono rapidamente seguendo un declino bifasico dopo entrambe le somministrazioni ia e s.c. L'AUC e la t _1/2 beta dopo una singola iniezione di 1 mg/kg ia e 2 mg/kg s.c. di questo composto sono rispettivamente 0,66 vs 1,2 μg × h/mL e 3,5 vs 4,5 ore.
Riferimenti	[1] https://pubmed.ncbi.nlm.nih.gov/21679466/ [2] https://pubmed.ncbi.nlm.nih.gov/9619762/ [3] https://pubmed.ncbi.nlm.nih.gov/20553795/ [4] https://pubmed.ncbi.nlm.nih.gov/19175384/ [5] https://pubmed.ncbi.nlm.nih.gov/20001707/ [6] https://pubmed.ncbi.nlm.nih.gov/19326772/ [7] https://pubmed.ncbi.nlm.nih.gov/12373351/

Informazioni sullo studio clinico

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

Numero NCT	Reclutamento	Condizioni	Sponsor/Collaboratori	Data di inizio	Fasi
NCT05797740	Recruiting	Multiple Sclerosis	Merck Healthcare KGaA Darmstadt Germany an affiliate of Merck KGaA Darmstadt Germany	August 3 2023	--
NCT04997148	Completed	Relapsing-Remitting Multiple Sclerosis	Merck Healthcare KGaA Darmstadt Germany an affiliate of Merck KGaA Darmstadt Germany\|Merck Serono Limited an affiliate of Merck KGaA Darmstadt Germany	August 11 2021	--

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Cladribine Adenosine Deaminase inibitore

Struttura chimica

Peso molecolare: 285.69