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SEL120-34A HCl is a selective, orally available and ATP-competitive inhibitor of CDK8(CDK8/CycC and CDK19/CycC with IC50s of 4.4 nM and 10.4 nM , respectively), with antitumor activity.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $54 | In Stock | |
5 mg | $128 | In Stock | |
10 mg | $213 | In Stock | |
25 mg | $359 | In Stock | |
50 mg | $535 | In Stock | |
100 mg | $763 | In Stock | |
500 mg | $1,550 | In Stock |
Description | SEL120-34A HCl is a selective, orally available and ATP-competitive inhibitor of CDK8(CDK8/CycC and CDK19/CycC with IC50s of 4.4 nM and 10.4 nM , respectively), with antitumor activity. |
Targets&IC50 | CDK19-CyclinA:10.4 nM (IC50), CDK8-CyclinC:4.4 nM (IC50), CDK9-CyclinT:1070 nM (IC50) |
In vitro | SEL120-34A HCl is a selective, ATP-competitive inhibitor of CDK8(IC50 of 4.4 nM and 10.4 nM for CDK8/CycC and CDK19/CycC, respectively). SEL120-34A HCl is active against a panel of AML cell lines (GI50<1 μM), such as SKNO-1, KG-1, HEL-60, MOLM-16, MV-4-11, OciAML-2, MOLM-6 and OciAML-3 cells, consistent with the effective inhibition range of STAT1 S727 and STAT5 S726. |
In vivo | The growth of tumor in mice bearing MV4-11 cancer cells inhibited by SEL120-34A (30, 60 mg/kg, p.o.), and also arrests the growth of KG-1-derived tumors at 30 mg/kg via oral administration. |
Molecular Weight | 450.6 |
Formula | C15H19Br2ClN4 |
Cas No. | 1609452-30-3 |
Smiles | Cl.Cc1c(Br)c(Br)c2CCCn3c(nc1c23)N1CCNCC1 |
Relative Density. | no data available |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||
Solubility Information | DMSO: 8.33 mg/mL (18.49 mM), Sonication is recommended. | ||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||
DMSO
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