PKC412 ( CGP-41231 | CGP-41251 | Midostaurin | PKC-412 )

产品货号. M10759 CAS No. 120685-11-2

Midostaurin (PKC412; CGP 41251) 是一种具有口服活性的可逆多靶点蛋白激酶抑制剂。Midostaurin 抑制 PKCα/β/γ、Syk、Flk-1、Akt、PKA、c-Kit、c-Fgr、c-Src、FLT3、PDFRβ 和 VEGFR1/2，IC50 范围为 22-500 nM。Midostaurin 还上调内皮一氧化氮合酶 (eNOS) 基因表达。Midostaurin 显示出强大的抗癌作用。

纯度: >98% (HPLC)

COA

Datasheet

HNMR

HPLC

MSDS

Handing Instructions

规格	价格/人民币	库存	数量
5MG	￥648	有现货
10MG	￥1037	有现货
25MG	￥1847	有现货
50MG	￥2795	有现货
100MG	￥4155	有现货
500MG	￥9315	有现货
1G	获取报价	有现货

产品询价大包装询价加入购物车

生物学信息

产品名称

PKC412
注意事项

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断
产品简述

Midostaurin (PKC412; CGP 41251) 是一种具有口服活性的可逆多靶点蛋白激酶抑制剂。Midostaurin 抑制 PKCα/β/γ、Syk、Flk-1、Akt、PKA、c-Kit、c-Fgr、c-Src、FLT3、PDFRβ 和 VEGFR1/2，IC50 范围为 22-500 nM。Midostaurin 还上调内皮一氧化氮合酶 (eNOS) 基因表达。Midostaurin 显示出强大的抗癌作用。
产品描述

A potent, selective PKC inhibitor with IC50 of 50 nM; displays a high degree of selectivity over PKA (IC50=2.4 uM), S6 kinase (IC50=5.0 uM) and EGFR (IC50=3.0 uM) compared with Staurosporine; inhibits human brain tumors cells (mean IC50=0.4 uM), displays antitumor activity in vivo.Blood Cancer Phase 3 Clinical(In Vitro):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.(In Vivo):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.
体外实验

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体内实验

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同义词

CGP-41231 | CGP-41251 | Midostaurin | PKC-412
通路

Angiogenesis
靶点

PKC
受体

PKCα|PKCβ1|PKCβ2|PKCγ|PPK
研究领域

Cancer
适应症

Blood cancer

化学信息

CAS Number

120685-11-2
分子量

570.6371
分子式

C35H30N4O4
纯度

>98% (HPLC)
溶解度

DMSO: ≥ 21 mg/mL
SMILES

C[C@@]12[C@H](OC)[C@H](N(C(C3=CC=CC=C3)=O)C)C[C@H](N4C5=CC=CC=C5C6=C7C(CNC7=O)=C8C9=CC=CC=C9N2C8=C64)O1
化学全称

Benzamide, N-[(9S,10R,11R,13R)-2,3,10,11,12,13-hexahydro-10-methoxy-9-methyl-1-oxo-9,13-epoxy-1H,9H-diindolo[1,2,3-gh:3',2',1'-lm]pyrrolo[3,4-j][1,7]benzodiazonin-11-yl]-N-methyl-

运输与储存

储存条件

(-20℃)
运输条件

With Ice Pack
稳定性

≥ 2 years

参考文献

1. Meyer T, et al. Int J Cancer. 1989 May 15;43(5):851-6. 2. Krause KH, et al. Eur J Pharmacol. 1992 Oct 1;227(2):221-4. 3. Amon U, et al. Pharmacology. 1993 Sep;47(3):200-8. 4. Begemann M, et al. Clin Cancer Res. 1996 Jun;2(6):1017-30.

计算器

浓度计算器

摩尔计算器

分子量计算器

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