同义名 :	K0706; SCO-088; SUN-K0706; SUN K706
	CAS号 :	1388803-90-4
	货号 :	A1477196
	分子式 :	C27H20ClN3O2
	纯度 :	99%+
	分子量 :	453.92
	MDL号 :	MFCD34167514
	存储条件：	Pure form Sealed in dry, 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-ABL1 plays a key role in the pathogenesis of chronic myeloid leukemia (CML), and it has been investigated as a druggable target of tyrosine kinase inhibitors (TKIs) over two decades[1].Vodobatinib (K0706, SCO-088, SUN K706, SUN-K0706) is a novel BCR-ABL1 tyrosine kinase inhibitor with an IC50 of 7 nM. Vodobatinib exhibits activity against most BCR-ABL1 point mutants with IC50s of 167 nM, 154 nM,165 nM and 1967 nM for BCR-ABL1L248R, BCR-ABL1Y253H , BCR-ABL1E255V and BCR-ABL1T315I, respectively. K0706 was designed as a BCR-ABL1 TKI to provide an option for patients experiencing resistance or intolerance to the first-line TKIs imatinib, nilotinib, dasatinib, and bosutinib[2].Potent inhibition of BCR-ABL1 tyrosine autophosphorylation by K0706 as well as inhibition of BCR-ABL1L248R, BCR-ABL1Y253H and BCR-ABL1E255V at high concentrations of inhibitor. BCR-ABL1T315I was not inhibited to a level reaching the IC50 at any of the tested concentrations of K0706[3].

实验方案
	1mg	5mg	10mg
1 mM 5 mM 10 mM	2.20mL 0.44mL 0.22mL	11.02mL 2.20mL 1.10mL	22.03mL 4.41mL 2.20mL

参考文献

[1] Hyewon Lee 1 , Igor Novitzky Basso, Dennis Dong Hwan Kim.Target spectrum of the BCR-ABL tyrosine kinase inhibitors in chronic myeloid leukemia. [2] . Cortes JE, Gambacorti-Passerini C, Deininger MW, et al. Bosutinib Versus Imatinib for Newly Diagnosed Chronic Myeloid Leukemia: Results From the Randomized BFORE Trial. Journal of clinical oncology : official journal of the American Society of Clinical Oncology 2018;36:231–237 [3]Orlando Antelope, Nadeem A Vellore,et al. BCR-ABL1 tyrosine kinase inhibitor K0706 exhibits preclinical activity in Philadelphia chromosome-positive leukemia. Exp Hematol.2019 Sep;77:36-40.e2.