(S)-3-Hydroxy Midostaurin

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CAS NO:

945260-14-0

(S)-CGP52421

(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。

生物活性	(S)-3-Hydroxy Midostaurin ((S)-CGP52421) is a potent kinases inhibitor withIC₅₀values of<400 nm for 13 kinases (vegfr-2, trk-a,FLT3, et). (S)-3-Hydroxy Midostaurin is a minor metabolite of midostaurin (PKC412; HY-10230) undergoing by the hepatic CYP3A4 enzyme. (S)-3-Hydroxy Midostaurin has the potential for acute myeloid leukemia (AML)^[1].
体外研究 (In Vitro)	(S)-3-Hydroxy Midostaurin ((S)-CGP52421; compound 4) has IC₅₀values in the range of 200-400 nM against the ITD and D835Y mutants and low micromolar activity against the wild-type enzyme^[1]. The epimeric mixture of metabolites ((R)-3-Hydroxy Midostaurin + (S)-3-Hydroxy Midostaurin) substantially inhibits the proliferation of only the Tel-PDGFRβ (GI₅₀=63 nM), KIT D816V (GI₅₀=320 nM), and FLT3-ITD (GI₅₀=650 nM) BaF3 cell lines, while the wild-type cells are relatively insensitive^[1].
分子量	586.64
Formula	C₃₅H₃₀N₄O₅
CAS 号	945260-14-0
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Please store the product under the recommended conditions in the Certificate of Analysis.