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G1T38

Chemical Structure : G1T38

CAS No.: 1628256-23-4

G1T38 (Lerociclib;G1T 38)

Catalog No.: PC-60397Not For Human Use, Lab Use Only.

G1T38 (Lerociclib, G1T 38) is a novel, potent and selective inhibitor of CDK4/6 with biochemical IC50 of 1 nM and 2 nM for CDK4/cyclin D1 and CDK6/cyclin D3, respectively.

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

Biological Activity

G1T38 (Lerociclib, G1T 38) is a novel, potent and selective inhibitor of CDK4/6 with biochemical IC50 of 1 nM and 2 nM for CDK4/cyclin D1 and CDK6/cyclin D3, respectively.
G1T38 (Lerociclib) shows weak inhibitory effect on CDK9/cyclin T (IC50=28 nM) and CDK5/p35 (IC50=832 nM), >1,000-fold selectivity over CDK1/2/7.
G1T38 (Lerociclib) decreases RB1 phosphorylation, causes G1 arrest, and inhibits cell proliferation in a variety of CDK4/6-dependent tumorigenic cell lines.
G1T38 (Lerociclib, demonstrates equivalent or improved tumor efficacy compared to palbociclib in an ER+ breast cancer xenograft model.

Physicochemical Properties

M.Wt 474.613
Formula C26H34N8O
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-isopropylpiperazin-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. Oncotarget. 2017 Jun 27;8(26):42343-42358.

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

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