G-749 is a FLT3 inhibitor that showed potent and sustained inhibition of the FLT3 wild type and mutants with IC50s of 0.4/0.6/3.5/7.5 nM for Wt Flt3/D835Y/MV4-11/Molm-14 respectively.
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产品名称 | FLT3 ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
R406 | ✔ | Syk | 99%+ | ||||||||||||||||
Go6976 | ✔ | 99%+ | |||||||||||||||||
Quizartinib |
+++
FLT3 (WT), IC50: 4.2 nM FLT3 (ITD), IC50: 1.1 nM |
99%+ | |||||||||||||||||
Gilteritinib |
++++
FLT3, IC50: 0.29 nM |
99%+ | |||||||||||||||||
Amuvatinib |
+
FLT3 (D835Y), IC50: 81 nM |
99%+ | |||||||||||||||||
Pacritinib |
++
FLT3, IC50: 22 nM FLT3 (D835Y), IC50: 6 nM |
97% | |||||||||||||||||
Dovitinib |
++++
FLT3, IC50: 1 nM |
c-Kit | 99%+ | ||||||||||||||||
Denfivontinib |
++++
FLT3, IC50: 0.4 nM FLT3 (D835Y), IC50: 0.4 nM |
RET | 99%+ | ||||||||||||||||
TAK-659 HCl |
++
FLT3, IC50: 4.6 nM |
Syk | 99%+ | ||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
靶点 |
|
描述 | Acute myeloid leukemia (AML) is an aggressive hematologic disorder in which the hematopoietic progenitor cells lose their ability to differentiate normally and continue to proliferate. Fms-like tyrosine receptor kinase (FLT) 3 plays an important role in normal hematopoiesis and leukemogenesis and is expressed in most AML blasts. G-749 is a novel and effective FLT3 inhibitor with IC50s of 0.4 nM, 0.6 nM and 1 nM for FLT3 (WT), FLT3 (D835Y) and Mer, respectively. G-749 inhibited autophosphorylation of FLT3 with an IC50 value of ≤8 nM in FLT3-WT bearing RS4-11 and in FLT3-ITD harboring MV4-11 and Molm-14 cells. The antiproliferative activity of G-749 was assessed in several leukemia cell lines where it showed strong antiproliferation of leukemia cells addicted to FLT3-ITD (MV4-11 and Molm-14) in a dose-dependent manner. The BaF3 cells expressing the indicated FLT3 mutations were incubated for 2 h with G-749, and G-749 showed strong potency against autophosphorylation of all tested FLT3 mutants with IC50 of <10 nM. A single dose of G-749 HCl salt (10 mg/kg) was administered orally to subcutaneous MV4-11 xenograft mice and showed sustained inhibition of p-FLT3, p-STAT5, and p-ERK1/2, which indicated that G-749 effectively inhibits the FLT3 pathway and that its inhibition lasts for 24 h. Antitumor efficacy was examined with the MV4-11 xenograft mice using G-749 HCl salt (administered orally every day for 28 days). Significant inhibition of tumor growth was observed in the 3 mg/kg per day dosing group from 4 days onward, and apparent tumor regression was seen in the 10 and 30 mg/kg per day dosing group[2]. |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
1.92mL 0.38mL 0.19mL |
9.59mL 1.92mL 0.96mL |
19.18mL 3.84mL 1.92mL |
CAS号 | 1457983-28-6 |
分子式 | C25H25BrN6O2 |
分子量 | 521.409 |
别名 | G-749 |
运输 | 蓝冰 |
存储条件 |
粉末 Keep in dark place,Inert atmosphere,Room temperature 液体 -20°C:3-6个月-80°C:12个月 |
溶解度 |
DMSO: 25 mg/mL(47.95 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |