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描述 | HPK1-IN-7 is a potent and orally active inhibitor of HPK1 (hematopoietic progenitor kinase 1, MAP4K1), exhibiting an IC50 of 2.6 nM, along with remarkable family and kinome selectivity. It demonstrates selectivity against IRAK4 (59 nM) and GLK (140 nM), and exhibits robust efficacy in the MC38 syngeneic tumor model when combined with anti-PD1 [1]. |
Animal study | HPK1-IN-7 (100 mg/kg; orally; twice daily for 28 days) significantly enhances the efficacy of anti-PD1 treatment in a colorectal cancer syngeneic tumor model [1].HPK1-IN-7 (1 mg/kg; intravenous; in mice) displays moderate plasma clearance (43 mL/min/kg) and a large volume of distribution (4.4 L/kg). After oral administration (20 mg/kg), it achieves a Cmax of 5.3 μM and an AUC0-24h of 19 μM•h. Based on these pharmacokinetic findings, the calculated oral bioavailability is approximately 100% [1]. |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
2.18mL 0.44mL 0.22mL |
10.91mL 2.18mL 1.09mL |
21.81mL 4.36mL 2.18mL |
CAS号 | 2320462-65-3 |
分子式 | C24H22N6O4 |
分子量 | 458.47 |
SMILES Code | O=C1OC(C)(C)C2=C1C=CC(NC3=NC=C(C4=NN=CO4)C(N[C@@H](C5=CC=CC=C5)CO)=N3)=C2 |
MDL No. | N/A |
别名 | CompK; compound K; HPK1-IN 7, HPK1-IN7 |
运输 | 蓝冰 |
InChI Key | RVSSNRBUPQUIEG-LJQANCHMSA-N |
Pubchem ID | 142587219 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Sealed in dry,2-8°C |
溶解方案 |
请根据您的动物给药指南选择适当的溶解方案。 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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