Chemical Structure : ZLC491
CAS No.:
3053716-46-1
ZLC491
(ZLC-491)
Catalog No.: PC-23155Not For Human Use, Lab Use Only.
ZLC491 is a potent, selective, and orally bioavailable CDK12/13 PROTAC degrader with DC50 values of 32 and 28 nM, respectively, in TNBC MDA-MB-231 cells.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
ZLC491 is a potent, selective, and orally bioavailable CDK12/13 PROTAC degrader with DC50 values of 32 and 28 nM, respectively, in TNBC MDA-MB-231 cells.
ZLC491 selectively induces CDK12/13 degradation in a cereblon- and proteasome-dependent manner.
ZLC491 is able to deplete CDK12/13 in a concentration-dependent manner in other TNBC cells including HCC38 and MDA-MB-436 cells.
ZLC491 is highly selective for CDK12 over other CDKs.
ZLC491 effectively reduces DDR gene expression and potently inhibited TNBC cell growth alone or combined with DNA damaging agents or PARP inhibitors.
ZLC491 potently inhibits the growth of MDA-MB-231, HCC38, and MDA-MB-436 cells with IC50 values of 0.62, 0.19 and 0.12 μM, respectively.
ZLC491 (100-200 mg/kg, p.o.) depleted CDK12 and CDK13 proteins, induced apoptotic cell death in the tumors in MDA-MB-231 xenografts model.
Physicochemical Properties
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M.Wt
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867.00
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Formula
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C48H51FN10O5
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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3-Benzyl-1-((1r,4r)-4-((5-cyanopyridin-2-yl)amino)cyclohexyl)-1-(4-(4-(1-(2-(2,6-dioxopiperidin-3-yl)-6-fluoro-1,3-dioxoisoindolin-5-yl)piperidin-4-yl)piperazin-1-yl)phenyl)urea
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References
1. Licheng Zhou, et al. J Med Chem. 2024 Oct 10. doi: 10.1021/acs.jmedchem.4c01596.
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