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PKC412
CAS No. 120685-11-2
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 | ￥1416 | 有现货 |
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| 10MG | ￥2261 | 有现货 |
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| 25MG | ￥3488 | 有现货 |
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| 50MG | ￥4957 | 有现货 |
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| 100MG | ￥6561 | 有现货 |
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| 200MG | ￥8865 | 有现货 |
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| 500MG | 获取报价 | 有现货 |
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| 1G | 获取报价 | 有现货 |
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| 1 mL x 10 mM in DMSO | ￥1777 | 有现货 |
|
生物学信息
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产品名称PKC412
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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
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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。
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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.
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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
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通路Angiogenesis
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靶点PKC
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受体PKCα|PKCβ1|PKCβ2|PKCγ|PPK
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研究领域Cancer
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适应症Blood cancer
化学信息
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CAS Number120685-11-2
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分子量570.6371
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分子式C35H30N4O4
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纯度>98% (HPLC)
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溶解度DMSO: ≥ 21 mg/mL
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SMILESC[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
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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
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储存条件(-20℃)
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运输条件With Ice Pack
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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.
