| 产品描述： | HPK1-IN-7 is a potent, orally active HPK1 (hematopoietic progenitor kinase 1, MAP4K1) inhibitor (IC50=2.6 nM) with excellent family and kinome selectivity. HPK1-IN-7 shows selectivity against IRAK4 (59 nM) and GLK (140 nM). HPK1-IN-7 shows robust efficacy against MC38 syngeneic tumor model in combination with anti-PD1 |
| 靶点： |
HPK1：2.6 nM (IC50)；GLK/MAP4K3：140 nM (IC50)；IRAK4：59 nM (IC50)；Fms/CSFR：3.2 nM (IC50)；FLT3：25.4 nM (IC50)；AMPKA1：44.3 nM (IC50)；cKIT：45.7 nM (IC50)；MST1：55.1 nM (IC50)；ICK：65.1 nM (IC50)；MST2：78.5 nM (IC50);MAPK |
| 体内研究： |
HPK1-IN-7 (compound 24) (100 mg/kg; p.o.; twice daily for 28 days) 在结直肠癌同系肿瘤模型中显示抗 PD1 功效的强劲增强。 HPK1-IN-7 (1 mg/kg; intravenous; mice) 的特点是血浆清除率适中 (43 mL/min/kg) 和分布容积大 (4.4 L/kg)。口服 (20 mg/kg) 后，Cmax 为 5.3 μM，AUC0-24h为 19 μM?h。根据这些药代动力学研究计算出的口服生物利用度约为 100%。 Animal Model: Mice (MC38 syngeneic tumor model) Dosage: 100 mg/kg Administration: Oral; twice daily for 28 days Result: Enhanced the efficacy of anti-PD1 treatment, garnering a 100% cure rate vs a 20% cure rate with anti-PD1 alone. |
| 参考文献： |
1. Degnan AP, et al. Discovery of Orally Active Isofuranones as Potent, Selective Inhibitors of Hematopoetic Progenitor Kinase 1. ACS Med Chem Lett. 2021;12(3):443-450. |
| 溶解性： |
Soluble in DMSO |
| 保存条件： |
-20℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.181 ml |
10.906 ml |
21.811 ml |
| 5 mM |
0.436 ml |
2.181 ml |
4.362 ml |
| 10 mM |
0.218 ml |
1.091 ml |
2.181 ml |
| 50 mM |
0.044 ml |
0.218 ml |
0.436 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京