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首页-小分子抑制剂&激动剂-Tyrosine Kinase-Src-RK-20449
RK-20449

Chemical Structure : RK-20449

CAS No.: 364042-47-7

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RK-20449 (RK20449, A419259, A-419259)

货号: PC-35754Not For Human Use, Lab Use Only.

RK-20449 (A419259) is a potent, small molecule inhibitor of hematopoietic cell kinase (HCK) with IC50 of 0.43 nM.

规格 价格 库存 数量
5 mg ￥1180 In stock
10 mg ￥1780 In stock
25 mg ￥2980 In stock
50 mg ￥4880 In stock
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

RK-20449 (A419259) is a potent, small molecule inhibitor of hematopoietic cell kinase (HCK) with IC50 of 0.43 nM.
RK-20449 displays an IC50 <100 nM against 7 kinases in a panel of 107 human kinases, all of which are SFKs (FYN, HCK, LCK, LYNa, LYNb, SRC, and YES), consistent with the high level of amino acid sequence homology among the SFKs.
RK-20449 potently inhibits CD34+ CD38− human primary AML cell proliferation to a greater extent than the known SFK inhibitor PP2, shows dose-dependent inhibition of leukemia stem cells (LSCs) proliferation with IC50 <1 uM in 17 of 25 AML cases.
RK-20449 significantly reduces human LSC and non-stem AML burden in vivo models.

物理化学性质&存储条件

分子量 481.644
分子式 C30H35N5O
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

7-(trans-4-(4-methylpiperidin-1-yl)cyclohexyl)-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine

参考文献

1. Saito Y, et al. Sci Transl Med. 2013 Apr 17;5(181):181ra52.

2. Poh AR, et al. Cancer Cell. 2017 Apr 10;31(4):563-575.e5.

3. Yuki H, et al. Bioorg Med Chem. 2017 Aug 15;25(16):4259-4264.

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