PRN1371
作者：齐岳
发布时间：2023-08-28
09:00:53
点击数：
产品名称：PRN1371
产品描述：
| 产品描述 | PRN1371 is a specific and potent FGFR1-4 and CSF1R inhibitor (IC50s: 0.6/1.3/4.1/19.3/8.1 nM for FGFR1/2/3/4 and CSF1R). |
| 靶点活性 | FGFR4:19.3 nM (IC50), FGFR3:4.1 nM (IC50), CSF1R:8.1 nM (IC50), FGFR1:0.6 nM (IC50), FGFR2:1.3 nM (IC50) |
| 体外活性 | PRN1371 presents a unique profile of high biochemical and cellular potency (FGFR1 IC50:0.6 nM, SNU16 IC50: 2.6 nM), prolonged target engagement (FGFR1 occupancy 24 h=96%), < 30% hERG inhibition at 1 μM, and good predicted ADME stability with BME reactivity Kd>100 μM. |
| 体内活性 | In PK studies of rat, dog, and cynomolgus monkey, PRN1371show rapid iv clearance in all species. PRN1371 shows rapid clearance (Cl=160 mL per min per kg), yet dosing p.o (20 mg/kg) demonstrates high oral exposure (AUC=4348 h·ng/mL) and a reasonable half-life (t1/2=3.8 h). Low levels of pFGFR2 confirm the ability of PRN1371 to block FGFR2 activity in tumor tissue. PRN1371 induces a dose-dependent reduction in tumor volume and up to 68% tumor growth inhibition at the highest dose of 10 mg/kg b.i.d. following 27 days of treatment. All doses are well tolerated with no significant bodyweight loss. |
| 分子量 | 561.46 |
| 分子式 | C26H30Cl2N6O4 |
| CAS No. | 1802929-43-6 |
存储
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 12 mg/mL (21.38 mM),Need ultrasonic and warming
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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公司介绍：
西安齐岳生物科技有限公司是集化学科研和定制与一体的高科技化学公司。业务范围包括化学试剂和产品的研发、生产、销售等。涉及产品为通用试剂的分销、非通用试剂的定制与研发，涵盖生物科技、化学品、中间体和化工材料等领域。
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