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Dasatinib hydrochloride

Catalog No. T22303 CAS 854001-07-3

Synonyms: BMS-354825 HCl

Dasatinib hydrochloride (BMS-354825 HCl) (BMS-354825) hydrochloride is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity. The Kis are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib hydrochloride hydrochloride inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively. Dasatinib hydrochloride hydrochloride also induces Apoptosis and Autophagy.

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Dasatinib hydrochloride Chemical Structure

Dasatinib hydrochloride, CAS 854001-07-3

Pack Size	Availability	Price/USD
50 mg	In stock	$ 38.00
100 mg	In stock	$ 54.00
1 mL * 10 mM (in DMSO)	In stock	$ 57.00

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Purity: 99.98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Dasatinib hydrochloride (BMS-354825 HCl) (BMS-354825) hydrochloride is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity. The Kis are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib hydrochloride hydrochloride inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively. Dasatinib hydrochloride hydrochloride also induces Apoptosis and Autophagy.
Targets&IC50	c-Kit (D816V):37 nM, Abl:0.6 nM, c-Kit (WT):79 nM, Src:0.8 nM
In vitro	Dasatinib hydrochloride demonstrates significant activity against Bcr-Abl, Src, Lck, Yes, c-Kit, PDGFRβ, p38, Her1, Her2, FGFR-1, and MEK with IC50s of <1.0, 0.50, 0.40, 0.50, 5.0, 28, 100, 180, 720, 880, and 1700 nM, respectively. Dasatinib hydrochloride shows antiproliferative activities aversus K562 chronic myelogenous leukemia (CML), PC3 human prostate tumor, MDA-MB-231 human breast tumor, and WiDr human colon tumor cell lines with IC50s of <1.0 nM, 9.4 nM, 12 nM, and 52 nM, respectively[1].
In vivo	Dasatinib hydrochloride (5 mg/kg and 50 mg/kg, qd×10d, 5 on-2 off) possesses potent antitumor activity and a high safety margin in a K562 xenograft model of chronic myelogenous leukemia (CML), demonstrating complete tumor regressions and low toxicity at multiple dose levels. Dasatinib hydrochloride (10 mg/kg) has a pharmacokinetic profile appropriate for continued advancement into in vivo efficacy studies. Dasatinib hydrochloride (10 mg/kg) demonstrates favorable half-lives (t1/2s) of 3.3 and 3.1 h for i.v. and oral, respectively. The oral bioavailability (Fpo) in this study is 27%[1].

Synonyms	BMS-354825 HCl
Molecular Weight	524.47
Formula	C22H27Cl2N7O2S
CAS No.	854001-07-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 13.5 mg/mL (25.7 mM), Sonification and heating are recommended.

References and Literature

1. Lombardo LJ, et al. Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Active Compound Library Anti-Cancer Approved Drug Library Inhibitor Library Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Drug Repurposing Compound Library EMA Approved Drug Library Tyrosine Kinase Inhibitor Library Bioactive Compound Library Cytoskeletal Signaling Pathway Compound Library

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Vamotinib Radotinib PD173955 SIAIS100 TFA Olverembatinib dimesylate Gypsogenin PPY A Lyn-IN-1

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Keywords

Dasatinib hydrochloride 854001-07-3 Angiogenesis Cytoskeletal Signaling Tyrosine Kinase/Adaptors Bcr-Abl Src c-Kit BMS-354825 HCl Dasatinib Hydrochloride inhibitor inhibit

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