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首页-小分子抑制剂&激动剂-Tyrosine Kinase-FLT3-HM43239
HM43239

Chemical Structure : HM43239

CAS No.: 2569527-64-4

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HM43239 (Tuspetinib, HM 43239)

货号: PC-20025Not For Human Use, Lab Use Only.

HM43239 (Tuspetinib, HM-43239) is a highly potent, selective FLT3 kinase inhibitor with IC50 of 1.1 nM, 1.8 nM and 1.0 nM aginst FLT3 WT, FLT3 ITD and FLT3 D835Y kinases, respectively.

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5 mg ￥980 In stock
10 mg ￥1580 In stock
25 mg ￥2780 In stock
50 mg ￥4880 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

HM43239 (Tuspetinib, HM-43239) is a highly potent, selective FLT3 kinase inhibitor with IC50 of 1.1 nM, 1.8 nM and 1.0 nM aginst FLT3 WT, FLT3 ITD and FLT3 D835Y kinases, respectively.
HM43239 showed high selectivity toward FLT3 and AML associated other kinases (e.g. SYK, JAK and TAK1) in 191 kinases biochemically assays.
HM43239 potently inhibited the growth of AML cell lines harboring FLT3 ITD mutation, such as MV4-11 (IC50: 1.3 nM), MOLM-13 (5.1 nM) and MOLM-14 (2.9 nM).
HM43239 effectively inhibited the phosphorylation levels of FLT3 and of downstream kinases related with cell proliferation, induced caspase 3/7-dependent apoptosis in AML cell lines expressing FLT3 ITD mutant.
HM43239 inhibited proliferation and induced apoptosis of leukemic stem cell (LSC) marker-expressing KG1a cells (CD34+/CD38- cells) suggesting that the possibility for targeting LSC.
HM43239 showed the excellent dose proportional antitumor activity in mouse models xenografted with both MV4-11 and MOLM-13 cell line without any significant toxicity.

物理化学性质&存储条件

分子量 501.08
分子式 C29H33ClN6
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

5-chloro-N-[3-cyclopropyl-5-[[(3R,5S)-3,5-dimethylpiperazin-1-yl]methyl]phenyl]-4-(6-methyl-1H-indol-3-yl)pyrimidin-2-amine

参考文献

1. Miyoung Lee, et.al. Cancer Res July 1 2018 (78) (13 Supplement) 804.

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