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AZD2932

CAS No. : 883986-34-3

MCE 站：AZD2932

产品活性：AZD2932是有效的多靶点激酶抑制剂，细胞试验中的抑制VEGFR2，PDGFβ，PDGFβ 和 PDGFβ 的 IC₅₀ 值分别为8，4，7，9 nM。

研究领域：Protein Tyrosine Kinase/RTK

作用靶点：PDGFR  |  VEGFR  |  FLT3  |  c-Kit

In Vitro: AZD2932 has a potent and balanced profile against PDGFβ, VEGFR-2, Flt-3 and c-Kit. It does not inhibit the various cytochrome P450 isoforms with the worst IC₅₀ being against 2C9 (8.0 μM). AZD2932 has no activity against hERG (IC₅₀=137 μM).

In Vivo: Twice daily oral dosing (b.i.d.) of AZD2932 10 h apart results in significant tumor growth inhibition of 64% for both 50 and 12.5 mg/kg doses on the day the control animals are terminated. Xenografts bearing non PDGFβ expressing tumor cells are also sensitive to AZD2932 treatment: growth of Calu-6 tumor is inhibited by 81% and 72% at 50 and 12.5 mg/kg b.i.d. and and LoVo tumors by 67% at 50 mg/kg b.i.d. This is due AZD2932 potent activity against VEGFR2 as well as a potential effect on pericytes and tumor-associated fibroblasts due to PDGFR a and b inhibition. AZD2932 at 3–50 mg/kg b.i.d. 10 h apart gives 60–80% inhibition of both p-VEGFR2 and p-PDGFβ in a 1:1 ratio.

相关产品：Bioactive Compound Library Plus  |  Kinase Inhibitor Library  |  Protein Tyrosine Kinase Compound Library  |  Anti-Cancer Compound Library  |  Differentiation Inducing Compound Library  |  Reprogramming Compound Library  |  Anti-Breast Cancer Compound Library  |  Anti-Pancreatic Cancer Compound Library  |  Anti-Blood Cancer Compound Library  |  Bevacizumab  |  Sunitinib  |  Imatinib  |  Semaxinib  |  SU 5402  |  PD173074  |  5Z-7-Oxozeaenol  |  Cediranib  |  SAR131675  |  AT9283  |  Gandotinib  |  KW-2449  |  GW806742X  |  Tanshinone IIA  |  Lestaurtinib  |  PF-03814735  |  Vatalanib dihydrochloride  |  CP-547632  |  CG-806  |  AST 487  |  Tyrphostin A9  |  Ki20227  |  Motesanib  |  SU14813  |  Ramucirumab  |  SU1498  |  MAZ51  |  PP121

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