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FRAX597

CAS No. : 1286739-19-2

MCE 站：FRAX597

产品活性：FRAX597 是一种有效的 I型 P21激活激酶 (PAK)抑制剂，作用于 PAK1，2 和 3，IC₅₀ 分别为 8，13 和 19 nM。

研究领域：Cell Cycle/DNA Damage  |  Cytoskeleton

作用靶点：PAK

In Vitro: FRAX597 is determined to be a potent, ATP-competitive inhibitor of group I PAKs (PAK 1-3), with biochemical IC₅₀ values as follows: PAK1 IC₅₀=8 nM, PAK2 IC₅₀=13 nM, PAK3 IC₅₀=19 nM. The IC₅₀ toward 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 IC₅₀ value of 48 nM against wild type PAK1, while IC₅₀ values against the V342F and V342Y PAK1 mutants are higher than 3 μM and 2 μM, respectively.

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).

相关产品：Bioactive Compound Library Plus  |  Cell Cycle/DNA Damage Compound Library  |  Kinase Inhibitor Library  |  Anti-Cancer Compound Library  |  Anti-Aging Compound Library  |  Cytoskeleton Compound Library  |  Fingolimod hydrochloride  |  IPA-3  |  5-Aminosalicylic Acid  |  FRAX486  |  NVS-PAK1-1  |  G-5555  |  GNE 2861  |  FRAX1036  |  LCH-7749944  |  Mesalamine impurity P  |  NVS-PAK1-C

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