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SEL120-34A is a selective and ATP-competitive inhibitor of CDK8 with IC50s of 4.4 nM, 10.4 nM and 1070 nM for CDK8/CycC, CDK19/CycC and CDK9/cycT. SEL120-34A possesses antitumor activity.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $58 | In Stock | |
5 mg | $167 | In Stock | |
10 mg | $251 | In Stock | |
25 mg | $417 | In Stock | |
50 mg | $593 | In Stock | |
100 mg | $798 | In Stock |
Description | SEL120-34A is a selective and ATP-competitive inhibitor of CDK8 with IC50s of 4.4 nM, 10.4 nM and 1070 nM for CDK8/CycC, CDK19/CycC and CDK9/cycT. SEL120-34A possesses antitumor activity. |
Targets&IC50 | CDK19-CyclinA:10.4 nM, CDK9-CyclinT:1070 nM, CDK8-CyclinC:4.4 nM |
In vitro | SEL120-34A shows no obvious inhibition on CDK1, 2, 4, 6, 5, 7. SEL120-34A weakly suppresses CDK9 with an IC50 of 1070 nM. SEL120-34A is active against a panel of AML cell lines including KG-1, SKNO-1, HEL-60, MOLM-16, OciAML-2, MV-4-11, MOLM-6 and OciAML-3 cells with GI50<1 μM[1]. |
In vivo | SEL120-34A (30 mg/kg and 60 mg/kg; p.o.) inhibits the growth of tumors in mice bearing MV4-11 cancer cells. SEL120-34A (30 mg/kg; p.o.) arrests the growth of KG-1-derived tumors[1]. |
Molecular Weight | 414.14 |
Formula | C15H18Br2N4 |
Cas No. | 1609522-33-9 |
Smiles | CC1=C2C=3N(C(=N2)N4CCNCC4)CCCC3C(Br)=C1Br |
Relative Density. | 1.92 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||
Solubility Information | DMSO: 4.14 mg/mL (10 mM) | ||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||
DMSO
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