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BPI-16350

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

M.Wt 518.62
Formula C28H32F2N8
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

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

References

1. Jian Zhang, et al. 2023 ASCO Annual Meeting I

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