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Chemical Structure : G1T38 dihydrochloride
CAS No.: 2097938-59-3
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.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $118 | In stock | |
| 10 mg | $188 | In stock | |
| 25 mg | $298 | In stock | |
| 50 mg | $488 | In stock | |
| 100 mg | Get quote |
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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.
| M.Wt | 547.529 | |
| Formula | C26H36Cl2N8O | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| 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 |
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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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