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首页-小分子抑制剂&激动剂-Tyrosine Kinase-FLT3-FF-10101
FF-10101

Chemical Structure : FF-10101

CAS No.: 1472797-69-5

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FF-10101 (FF10101)

货号: PC-38618Not For Human Use, Lab Use Only.

FF-10101 (FF10101) is a potent, selective, and irreversible FLT3 inhibitor with IC50 of 0.14 nM (FLT3 Wt), covalently binds to the C695 residue of FLT3.

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25 mg ￥3280 In stock
50 mg ￥5280 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

FF-10101 (FF10101) is a potent, selective, and irreversible FLT3 inhibitor with IC50 of 0.14 nM (FLT3 Wt), covalently binds to the C695 residue of FLT3.
FF-10101 potently inhibited the phosphorylation of FLT3-ITD than that of FLT3-ITD-C695S (IC50 values 2.4 nM and 79 nM, respectively).
FF-10101 potently and selectively inhibits the growth of mutant FLT3-expressing leukemia cells in vitro (MV4-11 c ell, IC50=0.83 nM), potently inhibits kinase activities of wild-type FLT3 and FLT3-D835Y with IC50 values of 0.20 nM and 0.16 nM, respectively.
FF-10101 demonstrated high kinase selectivity to wild-type FLT3 with >30-fold margins against the other kinases except for FMS and KIT with IC50 values of 0.94 nM and 2.0 nM, respectively.
FF-10101 showed growth inhibitory effects on all tested types of FLT3-TKD mutation- and FLT3-ITD with D835Y, Y842C, Y842H, or F691L mutation-expressing 32D cells with GI50 values from 0.43 nM to 6.1 nM.
FF-10101 (2, 5, and 10 mg/kg) demonstrated anti-leukemic effects in in vivo models, FF-10101 more potently inhibited the growth of tumors with FLT3-ITD-D835Y and FLT3-ITD-F691L than quizartinib.

物理化学性质&存储条件

分子量 530.677
分子式 C29H38N8O2
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

(2E)-N-[(1S)-2-[[5-[2-[(4-Cyanophenyl)amino]-4-(propylamino)-5-pyrimidinyl]-4-pentyn-1-yl]amino]-1-methyl-2-oxoethyl]-4-(dimethylamino)-N-methyl-2-butenamide

参考文献

1. Yamaura T, et al. Blood. 2018 Jan 25;131(4):426-438.

2. Ferng TT, et al. Mol Cancer Ther. 2022 Apr 8:OF1-OF11.

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