CAS NO: | 1286739-19-2 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
2mg | 电议 |
5mg | 电议 |
10mg | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
500mg | 电议 |
生物活性 | FRAX597 is a potent group I p21-activated Kinases (PAKs) inhibitor withIC50of 8, 13 and 19 nM forPAK1,2and3. | ||||||||||||||||
IC50& Target[1] |
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体外研究 (In Vitro) | FRAX597 is determined to be a potent, ATP-competitive inhibitor of group I PAKs (PAK 1-3), with biochemical IC50values as follows: PAK1 IC50=8 nM, PAK2 IC50=13 nM, PAK3 IC50=19 nM. The IC50toward PAK4, a member of group II PAKs is >10 μM. At a concentration of 100 nM FRAX597 displays a significant (>80% inhibition) inhibitory capacity toward YES1 (87%), RET (82%), CSF1R (91%), TEK (87%), PAK1 (82%), and PAK2 (93%). When measured using the Kinase Glo Assay in the presence of 20 nM protein and 1 μM ATP, FRAX597 displayed an IC50value of 48 nM against wild type PAK1, while IC50values against the V342F and V342Y PAK1 mutants are higher than 3 μM and 2 μM, respectively[1]. | ||||||||||||||||
体内研究 (In Vivo) | Analysis of the flux reading for the animals in the two cohorts demonstrates a significantly slower tumor growth rate in FRAX597-treated mice compared with control mice. After 14 days of treatment the animals are sacrificed and the tumors excised and weighed. FRAX597-treated cohort shows significantly lower average tumor weight compared with the control cohort (0.55 g versus 1.87 g, p=0.0001)[1]. | ||||||||||||||||
分子量 | 558.10 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C29H28ClN7OS | ||||||||||||||||
CAS 号 | 1286739-19-2 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
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溶解性数据 | In Vitro: DMSO : 14.29 mg/mL(25.60 mM;Need ultrasonic) 配制储备液
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以下溶剂前显示的百
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