KX2-391 is an inhibitor of Src with IC50 of 9 nM-60 nM in cancer cells. It is the first clinical and peptidomimetic class Src inhibitor.
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产品名称 | Fyn ↓ ↑ | Lck ↓ ↑ | Lyn ↓ ↑ | Src ↓ ↑ | Yes ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Saracatinib |
++
Fyn, IC50: 10 nM |
++++
LCK, IC50: <4 nM |
+++
Lyn, IC50: 5 nM |
++++
c-Src, IC50: 2.7 nM |
99%+ | ||||||||||||||
SU6656 |
+
Fyn, IC50: 170 nM |
+
Lyn, IC50: 130 nM |
+
Src, IC50: 280 nM |
++
YES, IC50: 20 nM |
98% | ||||||||||||||
PP1 |
+++
Fyn, IC50: 6 nM |
+++
LCK, IC50: 5 nM |
EGFR | 99%+ | |||||||||||||||
PP2 |
+++
Fyn, IC50: 5 nM |
++++
LCK, IC50: 4 nM |
98% | ||||||||||||||||
WH-4-023 |
++++
Lck, IC50: 2 nM |
+++
Src, IC50: 6 nM |
99%+ | ||||||||||||||||
NVP-BHG 712 |
+
c-Src, IC50: 1.266 μM |
99%+ | |||||||||||||||||
CCT196969 |
++
LCK, IC50: 0.02 μM |
+
Src, IC50: 0.03 μM |
98% | ||||||||||||||||
MNS |
+
Src, IC50: 29.3 μM |
Syk,p97 | 98% | ||||||||||||||||
Tirbanibulin |
++
Src (HuH7), GI50: 13 nM Src (Hep 3B), GI50: 26 nM |
99%+ | |||||||||||||||||
PP121 |
++
Src, IC50: 14 nM |
VEGFR,PDGFR | 99%+ | ||||||||||||||||
Bosutinib |
++++
Src, IC50: 1.2 nM |
99% | |||||||||||||||||
Dasatinib monohydrate |
++++
Src, IC50: 0.8 nM |
98% | |||||||||||||||||
Quercetin | ✔ | PKC,Sirtuin | 97% | ||||||||||||||||
Dasatinib |
++++
Src, IC50: 0.8 nM |
98% | |||||||||||||||||
Repotrectinib |
+++
Src, IC50: 5.3 nM |
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 | KX2-391, the first clinical Src inhibitor (peptidomimetic class) that targets the peptide substrate site of Src, with GI50 of 9-60 nM in cancer cell lines. |
细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 数据源 |
mouse NIH3T3 cells | Function assay | 3 days | Inhibition of constitutively active human c-SRC527F mutant-induced growth inhibition in mouse NIH3T3 cells after 3 days by MTT assay | 21852023 |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.32mL 0.46mL 0.23mL |
11.59mL 2.32mL 1.16mL |
23.17mL 4.63mL 2.32mL |
CAS号 | 897016-82-9 |
分子式 | C26H29N3O3 |
分子量 | 431.527 |
别名 | KX-01;KX2-391 |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Sealed in dry,Store in freezer, under -20°C |
溶解度 |
DMSO: 40 mg/mL(92.69 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 |
4% DMSO+30% PEG 300+water 5 mg/mL |