Chemical Structure : BPI-16350
CAS No.:
2397678-18-9
BPI-16350
(Tibremciclib, BPI 16350)
Catalog No.: PC-23058Not For Human Use, Lab Use Only.
BPI-16350 (Tibremciclib) is a highly potent, selective CDK4/6 inhibitor with IC50 of 2.21 nM and 0.4 nM for CDK4/cyclinD1 and CDK6/cyclinD1, with less inhibition of CDK9 (IC50=91.6 nM).
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
BPI-16350 (Tibremciclib) is a highly potent, selective CDK4/6 inhibitor with IC50 of 2.21 nM and 0.4 nM for CDK4/cyclinD1 and CDK6/cyclinD1, with less inhibition of CDK9 (IC50=91.6 nM).
BPI-16350 is far less active against other CDKs, such as CDK1/cyclinB, CDK2/cyclinE, CDK5/p25, and CDK7/cyclinH complexes.
BPI-16350 inhibits cell proliferation and viability by arresting cells at G1 phase.
BPI-16350 inhibited tumor growth by 71.7%, 89.5%, and 98.5% at dosages of 37.5, 75, and 150 mg/kg, respectively, in COLO 205 xenografts.
Physicochemical Properties
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M.Wt
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518.62
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Formula
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C28H32F2N8
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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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N-[5-[(4-Ethyl-1-piperazinyl)methyl]-2-pyridinyl]-5-fluoro-4-[(1R)-6-fluoro-1,2,3,4-tetrahydro-1-methylpyrido[1,2-a]benzimidazol-8-yl]-2-pyrimidinamine
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References
1. Jian Zhang, et al. 2023 ASCO Annual Meeting I
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