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抑制剂/激活剂

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凋亡与自噬

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Midostaurin 米哚妥林; PKC412; CGP 41251

Midostaurin (PKC412; CGP 41251) 是一种多靶点蛋白激酶抑制剂，抑制 PKCα/β/γ，Syk，Flk-1，Akt，PKA，c-Kit，c-Fgr，c-Src，FLT3，PDFRβ 和 VEGFR1/2 的 IC50 值范围为 22-500 nM。

货号：
TK0450
规格：

1mg

5mg

10mg
价格：
￥0.00

产品参数

CAS No.	120685-11-2
生物活性	Midostaurin (PKC412; CGP 41251) is a multi-targeted protein kinase inhibitor which inhibits PKCα/β/γ, Syk, Flk-1, Akt, PKA, c-Kit, c-Fgr, c-Src, FLT3, PDFRβ and VEGFR1/2 with IC50s ranging from 22-500 nM.
分子式	C35H30N4O4
分子量	570.64
运输条件	Room temperature in continental US; may vary elsewhere.
储存条件	-20°C, sealed storage, away from moisture
溶解性数据	DMSO : 50 mg/mL (87.62 mM; Need ultrasonic)
体内研究	Midostaurin (PKC412) strongly inhibits retinal neovascularization as well as laser-induced choroidal neovascularization in murine models. Midostaurin (PKC412) (25 mg/kg, i.p.) protects mouse livers of the K18 Arg90Cys-overexpressing transgenic mice from Fas-induced apoptosis.
体外研究	Midostaurin (PKC412) shows a broad antiproliferative activity against various tumor and normal cell lines in vitro, and is able to reverse the Pgp-mediated multidrug resistance of tumor cells in vitro. Exposure of cells to Midostaurin (PKC412) results in a dose-dependent increase in the G2/M phase of the cell cycle concomitant with increased polyploidy, apoptosis and enhanced sensitivity to ionizing radiation. Midostaurin (PKC412) induces substantial inhibition of KIT-, Lyn-, and STAT5 activity, but does not suppress Btk in HMC-1 cells and primary neoplastic mast cells. Midostaurin (PKC412) inhibits EN fusion tyrosine kinase in hematopoietic Ba/F3 cells. Midostaurin (PKC412) significantly inhibits EN phosphorylation in M0-91 and IMS-M2 cells in a dose-dependent manner.
文献	•Cell. 2018 Sep 20;175(1):171-185.e25. •Sci Transl Med. 2018 Jul 18;10(450). pii: eaaq1093. •Cancer Lett. 2020 Mar 31;473:130-138. •Haematologica. 2018 Nov;103(11):1862-1872. •Cancers. 2021 Feb 2;13(3):581. •Cancers. 2020 Jun 14;12(6):1574. •Br J Haematol. 2019 Nov;187(4):488-501. •J Cell Mol Med. 2020 Feb;24(3):2145-2156. •J Cell Mol Med. 2020 Mar;24(5):2968-2980. •Arch Toxicol. 2021 Jan;95(1):67-78. •Sci Rep. 2019 Dec 9;9(1):18630. •SLAS Discov. 2018 Aug;23(7):687-696. •Patent. US20200323850A1. •Department of Pharmacology & Toxicology. 2020 Jul.
纯度及产品资料	98%

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