3-Hydroxy Midostaurin(Synonyms: CGP52421)

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3-Hydroxy Midostaurin (Synonyms: CGP52421) 纯度: 97.02%

3-Hydroxy Midostaurin (CGP 52421) 是 PKC412 的代谢产物,可有效抑制 FMS 样酪氨酸激酶 3 (FLT3) 自磷酸化,在培养基和血浆中的 IC50 分别为 132 nM 和 9.8 μM。与 PKC412 相比,3-Hydroxy Midostaurin 的选择性较低,但细胞毒性更高。

3-Hydroxy Midostaurin(Synonyms: CGP52421)

3-Hydroxy Midostaurin Chemical Structure

CAS No. : 179237-49-1

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生物活性

3-Hydroxy Midostaurin (CGP 52421), a metabolite of PKC412, effectively inhibits FMS-like tyrosine kinase-3 (FLT3) autophosphorylation with IC50s of approximately 132 nM and 9.8 μM in culture medium and plasma, respectively. 3-Hydroxy Midostaurin is less selective but more cytotoxic than PKC412[1].

IC50 & Target

IC50: 132 nM (FLT3 in culture medium) and 9.8 μM (FLT3 in plasma)[1]

体外研究
(In Vitro)

CGP52421 (200, 400, 600, 800, 1000 nM) is more cytotoxic than PKC412 over the dose range 100 to 500 nM[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

586.64

Formula

C35H30N4O5

CAS 号

179237-49-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
参考文献
  • [1]. Levis M, et al. Plasma inhibitory activity (PIA): a pharmacodynamic assay reveals insights into the basis for cytotoxic response to FLT3 inhibitors. Blood. 2006 Nov 15;108(10):3477-83.

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