Chemical Structure : OKI-1546
CAS No.:
OKI-1546
(OKI1546, OKI 1546)
Catalog No.: PC-28533Not For Human Use, Lab Use Only.
OKI-1546 is a potent, selective, covalent and orally bioavailable CDK12/13 inhibitor with IC50 of 15 nM (CDK12), shows 649-, 81-, 11-, and 64-fold selective over CDKs 1, 2, 7, and 9, respectively.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
OKI-1546 is a potent, selective, covalent and orally bioavailable CDK12/13 inhibitor with IC50 of 15 nM (CDK12), shows 649-, 81-, 11-, and 64-fold selective over CDKs 1, 2, 7, and 9, respectively.
OKI-1546 potently inhibits proliferation of multiple cancer cell lines, with IC50 values that correlated with 50% inhibition of CTD pSer2.
OKI-1546 exhibits tumor growth inhibition in the BRCA1-mutant MDA-MB-436 tumor model in mice.
OKI-1546 induces a BRCAness phenotype and synergizes with merestinib in neuroblastoma (NB) cells and in vivo.
Physicochemical Properties
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M.Wt
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431.42
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Formula
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C21H20F3N5O2
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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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(R)-1-(5-(3-((5-(trifluoromethyl)pyrimidin-2-yl)amino)pyrrolidine-1-carbonyl)isoindolin-2-yl)prop-2-en-1-one
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References
1. Goulding JR, et al. Cell Rep. 2026 Oct 12;45(10):117997.
2. Alexander A. Strait, et al. Cancer Res (2023) 83 (7_Supplement): 1635.
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