MSC2530818 , 10mMinDMSO , 1883423-59-3
| Pack Size | Price | Stock | Quantity |
| 1ml | RMB395.20 | In Stock |
|
| others | Enquire |
PRODUCT Properties
| Boiling point: | 576.5±50.0 °C(Predicted) |
| Density | 1.373±0.06 g/cm3(Predicted) |
| storage temp. | Store at -20°C |
| solubility | DMF: 30 mg/ml; DMF:PBS (pH 7.2) (1:1): 0.50 mg/ml; DMSO: 15 mg/ml; Ethanol: 10 mg/ml |
| form | A crystalline solid |
| pka | 9.65±0.40(Predicted) |
| color | White to off-white |
| InChI | InChI=1S/C18H17ClN4O/c1-11-15-9-13(10-20-17(15)22-21-11)18(24)23-8-2-3-16(23)12-4-6-14(19)7-5-12/h4-7,9-10,16H,2-3,8H2,1H3,(H,20,21,22)/t16-/m0/s1 |
| InChIKey | ODRITQGYYWHQGM-INIZCTEOSA-N |
| SMILES | C(N1CCC[C@H]1C1=CC=C(Cl)C=C1)(C1=CN=C2NN=C(C)C2=C1)=O |
Description and Uses
MSC2530818 is an orally bioavailable cyclin-dependent kinase 8 (Cdk8) inhibitor (IC50 = 2.6 nM). It is selective for Cdk8 over a panel of 264 kinases at 1 μM but does inhibit glycogen synthase kinase 3α (GSK3α; IC50 = 691 nM). MSC2530818 inhibits STAT1 phosphorylation in SW620 colorectal cancer cells with an IC50 value of 8 nM. It also inhibits Wnt-dependent transcription in LS 174T, COLO 205, and PA-1 cancer cells (IC50s = 32, 9, and 52 nM, respectively, in luciferase reporter assays). MSC2530818 (50 and 100 mg/kg) reduces tumor growth in a SW620 mouse xenograft model.
MSC2530818 is a potent, selective and orally available CDK8 inhibitor with an IC50 of 2.6 nM for CDK8.
Safety
| Symbol(GHS) |  GHS07 |
| Signal word | Warning |
