1609522-33-9
1609522-33-9 structure
- Name: SEL120-34A
- Chemical Name: CDK8-IN-2
- CAS Number: 1609522-33-9
- Molecular Formula: C15H18Br2N4
- Molecular Weight: 414.14
- Catalog: Research Areas Cancer
- Create Date: 2018-01-23 02:57:02
- Modify Date: 2024-02-05 20:41:04
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SEL120-34A is a potent, selective, orally available, ATP-competitive CDK8 inhibitor, with IC50s of 4.4 nM and 10.4 nM for CDK8/CycC and CDK19/CycC, respectively, with antitumor activity.
| Name | CDK8-IN-2 |
|---|---|
| Synonyms | SEL120-34A |
| Description | SEL120-34A is a potent, selective, orally available, ATP-competitive CDK8 inhibitor, with IC50s of 4.4 nM and 10.4 nM for CDK8/CycC and CDK19/CycC, respectively, with antitumor activity. |
|---|---|
| Related Catalog | |
| Target |
CDK8/CycC:4.4 nM (IC50) CDK19/CycC:10.4 nM (IC50) CDK9/cycT:1070 nM (IC50) |
| In Vitro | SEL120-34A is a selective, ATP-competitive CDK8 inhibitor, with IC50 of 4.4 nM and 10.4 nM for CDK8/CycC and CDK19/CycC, respectively. SEL120-34A shows no obvious inhibition on CDK1, 2, 4, 6, 5, 7, and only weakly suppresses CDK9 (IC50, 1070 nM). SEL120-34A 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[1]. |
| In Vivo | SEL120-34A (30, 60 mg/kg, p.o.) inhibits the growth of tumor in mice bearing MV4-11 cancer cells, and also arrests the growth of KG-1-derived tumors at 30 mg/kg via oral administration[1]. |
| References |
| Molecular Formula | C15H18Br2N4 |
|---|---|
| Molecular Weight | 414.14 |