G1T38 ( Lerociclib;G1T 38 )

Catalog No. M12425 CAS No. 1628256-23-4

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Datasheet

HNMR

HPLC

MSDS

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Product Name

G1T38
Note

Research use only, not for human use.
Brief Description

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.
Description

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; 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; decreases RB1 phosphorylation, causes G1 arrest, and inhibits cell proliferation in a variety of CDK4/6-dependent tumorigenic cell lines; demonstrates equivalent or improved tumor efficacy compared to palbociclib in an ER+ breast cancer xenograft model.Breast Cancer,Phase 2 Clinical
Synonyms

Lerociclib;G1T 38
Pathway

Angiogenesis
Target

CDK
Recptor

CDK
Research Area

Cancer
Indication

Breast Cancer

CAS Number

1628256-23-4
Formula Weight

474.61
Molecular Formula

C26H34N8O
Purity

>98% (HPLC)
Solubility

——
SMILES

CC(C)N1CCN(CC1)C2=CN=C(C=C2)NC3=NC=C4C=C5C(=O)NCC6(N5C4=N3)CCCCC6
Chemical Name

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

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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