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1609452-30-3

1609452-30-3 structure
1609452-30-3 structure
  • Name: SEL120-34A hydrochloride
  • Chemical Name: SEL120-34A HCl
  • CAS Number: 1609452-30-3
  • Molecular Formula: C15H18Br2N4.xHCl
  • Molecular Weight:
  • Catalog: Research Areas Cancer
  • Create Date: 2018-11-18 08:21:33
  • Modify Date: 2024-09-21 07:57:10
  • SEL120-34A HCl 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 SEL120-34A HCl
Description SEL120-34A HCl 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 HCl 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 HCl shows no obvious inhibition on CDK1, 2, 4, 6, 5, 7, and only weakly suppresses CDK9 (IC50, 1070 nM). 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[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

[1]. Rzymski T, et al. SEL120-34A is a novel CDK8 inhibitor active in AML cells with high levels of serine phosphorylation of STAT1 and STAT5 transactivation domains. Oncotarget. 2017 May 16;8(20):33779-33795.

Molecular Formula C15H18Br2N4.xHCl
Storage condition 2-8℃