CHMFL-FLT3-122 (HYML-122, TR122)

Chemical Structure : CHMFL-FLT3-122

CAS No.: 1839150-56-9

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货号: PC-24328Not For Human Use, Lab Use Only.

CHMFL-FLT3-122 (HYML-122, TR122) is a potent, selective and orally active FLT3 kinase with IC50 of 40 nM, shows >10-fold selectivity over BTK (IC50=421 nM) and c-KIT (IC50=559 nM) kinases, also selectively targets RIPK2 kinase with IC50 of 14 nM.

规格	价格	库存
5 mg	￥1380	In stock
10 mg	￥2180	In stock
25 mg	￥3880	In stock
50 mg		Get quote
100 mg		Get quote

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生物&药学活性

CHMFL-FLT3-122 (HYML-122, TR122) is a potent, selective and orally active FLT3 kinase with IC50 of 40 nM, shows >10-fold selectivity over BTK (IC50=421 nM) and c-KIT (IC50=559 nM) kinases, also selectively targets RIPK2 kinase with IC50 of 14 nM.
CHMFL-FLT3-122 demonstrates 170-fold selectivity between FLT3 kinase and c-KIT kinase (GI50 = 11 nM versus 1900 nM) in the TEL-fusion isogenic BaF3 cells.
CHMFL-FLT3-122 induces apoptosis by arresting the cell cycle into the G0/G1 phase.
CHMFL-FLT3-122 significantly inhibits the proliferation of FLT3-ITD positive AML cancer cell lines MV4-11 (GI50 = 22 nM), MOLM13/14 (GI50 = 21 nM/42 nM).
CHMFL-FLT3-122 demonstrates a good bioavailability (30%) and significantly suppressed the tumor growth in MV4-11 cell inoculated xenograft model (50 mg/kg) without exhibiting obvious toxicity.

物理化学性质&存储条件

分子量	471.57
分子式	C26H29N7O2
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
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Solubility	10 mM in DMSO
Chemical Name/SMILES	1-[(3R)-3-[4-Amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl]-1-piperidinyl]-2-(dimethylamino)-ethanone

参考文献

1. Li X, et al. J Med Chem. 2015 Dec 24;58(24):9625-38.