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Senexin C is a novel orally active and specific CDK8/19 inhibitor with potential anticancer activity.Senexin C is more metabolically stable and potent than Senexin B. Senexin C inhibits the growth of MV4-11 leukaemia cells.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | 178 € | In Stock | |
5 mg | 454 € | In Stock | |
10 mg | 777 € | In Stock | |
25 mg | 1.605 € | In Stock | |
50 mg | 2.745 € | 8-10 weeks | |
1 mL x 10 mM (in DMSO) | 501 € | In Stock |
Description | Senexin C is a novel orally active and specific CDK8/19 inhibitor with potential anticancer activity.Senexin C is more metabolically stable and potent than Senexin B. Senexin C inhibits the growth of MV4-11 leukaemia cells. |
Targets&IC50 | CDK8-CyclinC:3.6 nM, CDK8-CyclinC:1.4 nM (Kd), CDK8-CyclinC:2.9 nM (Kd) |
In vitro | Senexin C exhibits high selectivity for CDK8 and CDK19, with similar Kd values of 55 nM and 44 nM respectively for ATP analog binding, while showing much higher Kd values for the other three non-target kinases (HASPIN: 1000 nM; MAP4K2: 940 nM; MYO3B: > 30,000 nM)[1]. |
In vivo | Tumor-bearing mice(CT26 tumor mode) received Senexin C via intravenous injection at 2.5 mg/kg or orally at 100 mg/kg, and compound concentrations in blood and tumors were measured by LC-MS/MS. The results indicated that Senexin C exhibits favorable tumor PK characteristics and low toxicity[1]. |
Molecular Weight | 449.55 |
Formula | C28H27N5O |
Cas No. | 2375554-02-0 |
Smiles | N#CC=1C=CC2=NC=CC(NCCC=3C=CC4=CC(=CC=C4C3)C(=O)N5CCN(C)CC5)=C2C1 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||
Solubility Information | DMSO: 20 mg/mL (44.49 mM), Sonication and heating are recommended. | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
DMSO
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