FLT3-IN-3 在低纳摩尔浓度下非常有效地抑制 FLT3-ITD 阳性 MV4-11 和 MOLM-13 细胞系的增殖 (GI50 值分别为 2 nM 和 1 nM)。
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产品名称 | FLT3 ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
R406 | ✔ | Syk | 99%+ | ||||||||||||||||
Go6976 | ✔ | 99%+ | |||||||||||||||||
Quizartinib |
+++
FLT3 (ITD), IC50: 1.1 nM FLT3 (WT), IC50: 4.2 nM |
99%+ | |||||||||||||||||
Gilteritinib |
++++
FLT3, IC50: 0.29 nM |
99%+ | |||||||||||||||||
Amuvatinib |
+
FLT3 (D835Y), IC50: 81 nM |
99%+ | |||||||||||||||||
Pacritinib |
++
FLT3 (D835Y), IC50: 6 nM FLT3, IC50: 22 nM |
97% | |||||||||||||||||
Dovitinib |
++++
FLT3, IC50: 1 nM |
c-Kit | 99%+ | ||||||||||||||||
Denfivontinib |
++++
FLT3 (D835Y), IC50: 0.4 nM FLT3, 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。 |
描述 | FLT3-IN-3 is very effective in inhibiting the proliferation of FLT3-ITD-positive MV4-11 and MOLM-13 cell lines at low nanomolar concentrations (GI50 values of 2 nM and 1 nM, respectively). At a concentration of less than 100 nM for 1 h, FLT3-IN-3 abolished the phosphorylation of STAT5 at the Y694 site, which is a key component of STAT5 phosphorylation. FLT3-IN-3 also reduced the phosphorylation of ERK1/2 (T202/Y204) and MEK1/2 (S217/221) in the MAPK cascade. FLT3-IN-3 also interfered with the PI3K/AKT pathway and reduced the phosphorylation of the AKT S473 site[ 1]. 1]. |
Animal study | Administered intraperitoneally at a dose of 10 mg/kg, FLT3-IN-3 sustained inhibition of FLT3 and STAT5 phosphorylation over 48 hours in the MV4-11 subcutaneous xenograft model[1]. |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
2.04mL 0.41mL 0.20mL |
10.19mL 2.04mL 1.02mL |
20.38mL 4.08mL 2.04mL |
CAS号 | 2229050-90-0 |
分子式 | C27H38N8O |
分子量 | 490.644 |
别名 | SAN50900 |
运输 | 蓝冰 |
存储条件 |
粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C 液体 -20°C:3-6个月-80°C:12个月 |
溶解度 |
DMSO: 250 mg/mL(509.53 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 |