SEL120-34A HCl |
| رقم الكتالوجGC32898 |
SEL120-34A HCl هو مثبط CDK8 قوي ، انتقائي ، متاح عن طريق الفم ، منافس لـ ATP ، مع IC50s من 4.4 نانومتر و 10.4 نانومتر لـ CDK8 / CycC و CDK19 / CycC ، على التوالي ، مع نشاط مضاد للأورام
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1609452-30-3
Sample solution is provided at 25 µL, 10mM.
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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.
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].
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].
[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.
Average Rating: 5 (Based on Reviews and 34 reference(s) in Google Scholar.)
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