生物活性 体外研究
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3 Hydroxy Midostaurin Epimer 1 (CGP52421 Epimer 1)

3 Hydroxy Midostaurin Epimer 1 (CGP52421 Epimer 1),945260-14-0,结构式
3 Hydroxy Midostaurin Epimer 1 (CGP52421 Epimer 1)
  • CAS号:945260-14-0
  • 英文名:3 Hydroxy Midostaurin Epimer 1 (CGP52421 Epimer 1)
  • 中文名:3 Hydroxy Midostaurin Epimer 1 (CGP52421 Epimer 1)
  • CBNumber:CB45864995
  • 分子式:C35H30N4O5
  • 分子量:586.64
  • MOL File:Mol file
3 Hydroxy Midostaurin Epimer 1 (CGP52421 Epimer 1)化学性质
  • 密度 :1.53±0.1 g/cm3(Predicted)
  • 酸度系数(pKa) :12.23±0.70(Predicted)

3 Hydroxy Midostaurin Epimer 1 (CGP52421 Epimer 1)性质、用途与生产工艺

  • 生物活性 (S)-3-Hydroxy Midostaurin ((S)-CGP52421) 是一种有效的激酶抑制剂,对 VEGFR-2,TRK-A,FLT3 等 13 种激酶的 IC50 值为 <400 nM。(S)-3-Hydroxy Midostaurin 是 Midostaurin (PKC412; HY-10230) 通过肝 CYP3A4 酶代谢的次要代谢产物。(S)-3-Hydroxy Midostaurin 具有潜在的用于急性髓细胞性白血病 (AML) 的潜力。
  • 体外研究

    (S)-3-Hydroxy Midostaurin ((S)-CGP52421; compound 4) has IC 50 values in the range of 200-400 nM against the ITD and D835Y mutants and low micromolar activity against the wild-type enzyme.
    The epimeric mixture of metabolites ((R)-3-Hydroxy Midostaurin + (S)-3-Hydroxy Midostaurin) substantially inhibits the proliferation of only the Tel-PDGFRβ (GI 50 =63 nM), KIT D816V (GI 50 =320 nM), and FLT3-ITD (GI 50 =650 nM) BaF3 cell lines, while the wild-type cells are relatively insensitive.

3 Hydroxy Midostaurin Epimer 1 (CGP52421 Epimer 1)上下游产品信息
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