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PKC 412 (Midostaurin)是一种广谱蛋白激酶抑制剂。抑制常规PKC亚型α/β/γ，PDFRβ，VEGFR2，Syk，Flk-1，Flt3，Cdk1/B，PKA，c-Kit，c-Fgr，c-Src，VEGFR1和EGFR。显示有效的抗肿瘤活性。
Targets
| Target | Value |
|---|---|
| PKCα | IC50: 22nM |
| PKCγ | IC50: 24nM |
| PKCβ1 | IC50: 30nM |
| PKCβ2 | IC50: 31nM |
| PPK | IC50: 38nM |
| KDR | IC50: 86nM |
| c-Syk | IC50: 95nM |
| PKCη | IC50: 160nM |
| PKCδ | IC50: 330nM |
| Flk1 | IC50: 390nM |
| CDK1/CyclinB | IC50: 570nM |
| PKA | IC50: 570nM |
| c-FGR | IC50: 790nM |
| c-Src | IC50: 800nM |
| FLT1 | IC50: 912nM |
| PLK1 | IC50: >1.0μM |
| p38 | IC50: >1μM |
| Tie-1 | IC50: >1μM |
| c-Met | IC50: >1μM |
| EGFR | IC50: 1.1μM |
| PKCε | IC50: 1.25μM |
| Myosin-lightchainkinase | IC50: 1.9μM |
| c-Lyn | IC50: 4.30μM |
| p70S6K | IC50: 5.0μM |
| CSK | IC50: 8.0μM |
| CDK4/CyclinD1 | IC50: >10μM |
| Junkinase | IC50: >10μM |
| Tie-2 | IC50: >10μM |
| FGFR1 | IC50: >10μM |
| v-Abl | IC50: >100μM |
| ERK1 | IC50: >200μM |
| CK1 | IC50: >200μM |
| CK2 | IC50: >200μM |
| PKB | IC50: >300μM |
| PKCζ | IC50: 465μM |
| In vitro (25°C) | DMSO | 90 mg/mL (157.72 mM) | |
| Water | Insoluble | ||
| Ethanol | Warmed: 18 mg/mL | ||
| In vivo | 5% DMSO+45% PEG 300+ddH2O | 3 mg/mL | |
|
* <1 mg/ml means slightly soluble or insoluble. * Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
|||
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.1 mM | 17.52 mL | 87.62 mL | 175.24 mL |
| 0.5 mM | 3.5 mL | 17.52 mL | 35.05 mL |
| 1 mM | 1.75 mL | 8.76 mL | 17.52 mL |
| 5 mM | 0.35 mL | 1.75 mL | 3.5 mL |
*The above data is based on the productmolecular weight 570.64. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 目录号 | A12650 |
|---|---|
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 570.64 |
| Formula | C35H30N4O4 |
| Purity | >99% |
| Storage | Store lyophilized at -20ºC, keep desiccated. |
| CAS No. | 120685-11-2 |
| Synonyms | CGP 41251, PKC412, PKC-412, CGP41251, CGP-41251 |
| SMILES | C[C@@]12[C@@H]([C@@H](C[C@@H](O1)N3C4=CC=CC=C4C5=C6C(=C7C8=CC=CC=C8N2C7=C53)CNC6=O)N(C)C(=O)C9=CC=CC=C9)OC |
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