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SEL120-34A hydrochloride
CAS No. 1609452-30-3
SEL120-34A hydrochloride( SEL 120-34A )
Catalog No. M12317 CAS No. 1609452-30-3
SEL120-34A is an ATP-competitive, selective, orally active CDK8 inhibitor that inhibits kinase activities of CDK8/CycC and CDK19/CycC complexes with IC50 of 4.4 nM and 10.4 nM, respectively.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 5MG | 115 | Get Quote |
|
| 10MG | 192 | Get Quote |
|
| 25MG | 323 | Get Quote |
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| 50MG | 482 | Get Quote |
|
| 100MG | 687 | Get Quote |
|
| 500MG | 1395 | Get Quote |
|
| 1G | Get Quote | Get Quote |
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Biological Information
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Product NameSEL120-34A hydrochloride
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NoteResearch use only, not for human use.
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Brief DescriptionSEL120-34A is an ATP-competitive, selective, orally active CDK8 inhibitor that inhibits kinase activities of CDK8/CycC and CDK19/CycC complexes with IC50 of 4.4 nM and 10.4 nM, respectively.
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DescriptionSEL120-34A is an ATP-competitive, selective, orally active CDK8 inhibitor that inhibits kinase activities of CDK8/CycC and CDK19/CycC complexes with IC50 of 4.4 nM and 10.4 nM, respectively; shows no significant inhibition on other members of the CDK family (200-fold over CDK9); inhibits phosphorylation of STAT1 S727 and STAT5 S726 in cancer cells, inhibits IFN- responsive genes expression in vitro; exhibits complete inhibitions of STAT1 S727 and STAT5 S726 in Colo-205 CRC xenograft tissues in mice (60mg/kg).
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In VitroSEL120-34A 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.
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In VivoSEL120-34A (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.
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SynonymsSEL 120-34A
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PathwayAngiogenesis
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TargetCDK
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RecptorCDK
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Research Area——
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Indication——
Chemical Information
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CAS Number1609452-30-3
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Formula Weight450.6
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Molecular FormulaC15H19Br2ClN4
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Purity>98% (HPLC)
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SolubilityDMSO : 62.5 mg/mL
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SMILESCC1=C2C3=C(CCCN3C(=N2)N4CCNCC4)C(=C1Br)Br.Cl
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Chemical Name7,8-Dibromo-9-methyl-2-piperazin-1-yl-5,6-dihydro-4H-imidazo[4,5,1-ij]quinoline hydrochloride
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1. Rzymski T, et al. Oncotarget. 2017 May 16;8(20):33779-33795.
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