Dasatinib hydrochloride

• CAT Number: I005127
• CAS Number: 854001-07-3
• Molecular Formula: C22H27Cl2N7O2S
• Molecular Weight: 524.47
• Purity: ≥95%
• Target: Src
• Solubility: DMSO: ≤ 15 mg/mL
• Storage: Store at -20°C
• IC50: ＜1 nM/0.8 nM(Abl/ Src); 79 nM/37 nM (c-Kit WT/c-Kit D816V) [1] [2]
• IUPAC Name: N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)piperazin-1-yl]-2-methylpyrimidin-4-yl]amino]-1,3-thiazole-5-carboxamide;hydrochloride
• InChI: InChI=1S/C22H26ClN7O2S.ClH/c1-14-4-3-5-16(23)20(14)28-21(32)17-13-24-22(33-17)27-18-12-19(26-15(2)25-18)30-8-6-29(7-9-30)10-11-31;/h3-5,12-13,31H,6-11H2,1-2H3,(H,28,32)(H,24,25,26,27);1H
• InChIKey: MSCGWICDJYLQOJ-UHFFFAOYSA-N
• SMILES: CC1=C(C(=CC=C1)Cl)NC(=O)C2=CN=C(S2)NC3=CC(=NC(=N3)C)N4CCN(CC4)CCO.Cl

Dasatinib(BMS-354825) hydrochloride (Cat.No:I005127) is a potent and dual Abl/ Src inhibitor used in the treatment of certain types of cancer, including chronic myeloid leukemia and Philadelphia chromosome-positive acute lymphoblastic leukemia. It targets multiple kinases involved in cell signaling pathways, inhibiting tumor growth and proliferation. 

Reference

[1]. O/’Hare T, et al. In vitro activity of Bcr-Abl inhibitors AMN107 and BMS-354825 against clinically relevant imatinib-resistant Abl kinase domain mutants. Cancer Res. 2005 Jun 1;65(11):4500-5.
[2]. Shah NP, et al. Dasatinib (BMS-354825) inhibits KITD816V, an imatinib-resistant activating mutation that triggers neoplastic growth in most patients with systemic mastocytosis. Blood. 2006 Jul 1;108(1):286-91.
[3]. Chan CM, et al. Targeted inhibition of Src kinase with dasatinib blocks thyroid cancer growth and metastasis. Clin Cancer Res. 2012 Jul 1;18(13):3580-91.
[4]. Dargart JL, et al. Dasatinib therapy results in decreased B cell proliferation, splenomegaly, and tumor growth in a murine model of lymphoma expressing Myc and Epstein-Barr virus LMP2A. Antiviral Res. 2012 Jul;95(1):49-56.