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G1T38 dihydrochloride

Chemical Structure : G1T38 dihydrochloride

CAS No.: 2097938-59-3

G1T38 dihydrochloride (Lerociclib)

Catalog No.: PC-60398Not For Human Use, Lab Use Only.

Lerociclib (G1T38) dihydrochloride is a 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

Lerociclib (G1T38) dihydrochloride is a 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.
Lerociclib (G1T38) 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.
Lerociclib (G1T38) decreases RB1 phosphorylation, causes G1 arrest, and inhibits cell proliferation in a variety of CDK4/6-dependent tumorigenic cell lines.
Lerociclib (G1T38) demonstrates equivalent or improved tumor efficacy compared to palbociclib in an ER+ breast cancer xenograft model.

Physicochemical Properties

M.Wt 547.529
Formula C26H36Cl2N8O
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 dihydrochloride

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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