Dasatinib hydrochloride

SKU: orb1704834

Description

Dasatinib hydrochloride is a potent, orally bioavailable dual inhibitor of Src and Bcr-Abl tyrosine kinases, with sub-nanomolar IC50 values. It induces apoptosis and autophagy and is widely used in cancer research, including in vitro studies of leukemia cell lines and in vivo xenograft models for investigating therapeutic mechanisms.

Research Area

Cardiovascular Research, Cell Biology, Signal Transduction

Key Properties

• CAS Number: 854001-07-3
• MW: 524.47
• Purity: 99.98% (May vary between batches)
• Formula: C₂₂H₂₇Cl₂N₇O₂S
• SMILES: Cl.Cc1nc(Nc2ncc(s2)C(=O)Nc2c(C)cccc2Cl)cc(n1)N1CCN(CCO)CC1
• Target: c-Kit,Apoptosis,Autophagy,Bcr-Abl,Src
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2.5 mg/mL (4.77 mM);DMSO:13.5 mg/mL (25.74 mM)

Bioactivity

• Target IC50:
  PDGFRβ:28 nM|yes:0.5 nM|MEK:1700 nM|Her2:710 nM|Abl:0.6 nM|lck:0.4 nM|FGFR1:880 nM|c-Kit (D816V):37 nM|p38:100 nM|Her1:180 nM|c-Kit (WT):79 nM|Src:0.8 nM
• 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%.
• 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.

Storage & Handling

• Storage: store under nitrogen | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Src, BcrAbl, BMS-354825 HCl, Abl, Dasatinib Hydrochloride, c-Kit (D816V), c-Kit (wt), cKit

Compound Identifiers

PubChem CID

11466607