同义名 :	盐酸达沙替尼 ;BMS-354825 hydrochloride; Dasatinib hydrochloride; BMS-354825 HCl
	CAS号 :	854001-07-3
	货号 :	A263536
	分子式 :	C22H27Cl2N7O2S
	纯度 :	99%+
	分子量 :	524.47
	MDL号 :	MFCD26960525
	存储条件：	Pure form Inert atmosphere,2-8°C In solvent -20°C:3-6个月-80°C:12个月
	溶解度 :	-
	动物实验配方：

生物活性

描述

Bcr-Abl is a constitutively activated tyrosine kinase that causes chronic myeloid leukemia (CML)[3]. Dasatinib, a dual Src-Abl kinase inhibitor, potently inhibits wild-type Abl kinase and all mutants except T315I over a narrow range (IC50 ≤ 1.7 nM) in a concentration-dependent manner. Dasatinib (IC50: 0.8 nM) displays 325-fold greater potency compared with STI571 against cells expressing wild-type Bcr-Abl in Ba/F3 cells[4]. Treatment with dasatinib blocked papillary thyroid cancer (PTC) tumor growth in an orthotopic model by more than 90% (P=0.0014). Adjuvant and posttreatment approaches with dasatinib significantly inhibited metastasis (P=0.016 and P=0.004, respectively)[5].

实验方案
	1mg	5mg	10mg
1 mM 5 mM 10 mM	1.91mL 0.38mL 0.19mL	9.53mL 1.91mL 0.95mL	19.07mL 3.81mL 1.91mL

参考文献

[1]Shah NP, Lee FY, 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. [2]O'Hare T, Walters DK, 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. [3]Druker BJ, Sawyers CL, Kantarjian H, Resta DJ, Reese SF, Ford JM, Capdeville R, Talpaz M. Activity of a specific inhibitor of the BCR-ABL tyrosine kinase in the blast crisis of chronic myeloid leukemia and acute lymphoblastic leukemia with the Philadelphia chromosome. N Engl J Med. 2001 Apr 5;344(14):1038-42. doi: 10.1056/NEJM200104053441402. Erratum in: N Engl J Med 2001 Jul 19;345(3):232. PMID: 11287973. [4]O'Hare T, Walters DK, Stoffregen EP, Jia T, Manley PW, Mestan J, Cowan-Jacob SW, Lee FY, Heinrich MC, Deininger MW, Druker BJ. 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. doi: 10.1158/0008-5472.CAN-05-0259. PMID: 15930265. [5]Chan CM, Jing X, Pike LA, Zhou Q, Lim DJ, Sams SB, Lund GS, Sharma V, Haugen BR, Schweppe RE. Targeted inhibition of Src kinase with dasatinib blocks thyroid cancer growth and metastasis. Clin Cancer Res. 2012 Jul 1;18(13):3580-91. doi: 10.1158/1078-0432.CCR-11-3359. Epub 2012 May 14. PMID: 22586301; PMCID: PMC3931551.