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Trilaciclib

Chemical Structure : Trilaciclib

CAS No.: 1374743-00-6

Trilaciclib (G1T28)

Catalog No.: PC-60395Not For Human Use, Lab Use Only.

Trilaciclib (G1T28) is a novel, potent and selective inhibitor of CDK4/6 with biochemical IC50 of 1 nM and 4 nM for CDK4/cyclin D1 and CDK6/cyclin D3, respectively.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Trilaciclib (G1T28) is a novel, potent and selective inhibitor of CDK4/6 with biochemical IC50 of 1 nM and 4 nM for CDK4/cyclin D1 and CDK6/cyclin D3, respectively.
Trilaciclib (G1T28) displays >30-fold selectivity for CDK4/cyclin D1 over CDK2/cyclin A, CDK2/cyclin E, CDK5/p25, CDK5/p35, and CDK7/cyclin H/Mat1, 50-fold over CDK9/cyclin T.
Trilaciclib (G1T28) reversibly pauses the cell cycle in the G1 phase in CDK4/6-dependent cell lines, protects CDK4/6-dependent cells from chemotherapy-induced damage in vitro.
Trilaciclib (G1T28) induces a reversible cell-cycle arrest in murine and canine HSPCs; attenuates chemotherapy-induced myelosuppression in vivo.

Physicochemical Properties

M.Wt 446.55
Formula C24H30N8O
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

2'-((5-(4-methylpiperazin-1-yl)pyridin-2-yl)amino)-7',8'-dihydro-6'H-spiro[cyclohexane-1,9'-pyrazino[1',2':1,5]pyrrolo[2,3-d]pyrimidin]-6'-one

References

1. Bisi JE, et al. Mol Cancer Ther. 2016 May;15(5):783-93.

2. He S, et al. Sci Transl Med. 2017 Apr 26;9(387). pii: eaal3986.

3. Stice JP, et al. Mol Cancer Res. 2017 Jun;15(6):660-669.

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