[CAS NO. 1628256-23-4]  G1T38

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PRODUCTS SPECIFICATIONS [1628256-23-4]

Store
Catalog
SLK-S8568
Brand
Selleck
CAS
1628256-23-4

DESCRIPTION [1628256-23-4]

Overview

MDL-
Molecular Weight474.60
Molecular FormulaC26H34N8O
SMILES-

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

1 mg5 mg10 mg
1 mM2.1070 mL10.5352 mL21.0704 mL
5 mM---
10 mM---
50 mM---

Description

G1T38 (Lerociclib) is a novel, potent, selective, and orally bioavailable inhibitor with IC50 values of 0.001 μM, 0.002 μM and 0.028 μM for CDK4, CDK6 and CDK9 respectively.

Targets

CDK4 [1]
(Cell-free assay)
CDK6 [1]
(Cell-free assay)
CDK9 [1]
(Cell-free assay)
1 nM2 nM28 nM

In vitro

G1T38 is highly potent and selective for CDK4/cyclin D1 and CDK6/cyclin D3 over CDK1, CDK2, CDK5 and CDK7 and their respective binding partners. In vitro, G1T38 decreases RB1 (RB) phosphorylation, causes a precise G1 arrest, and inhibits cell proliferation in a variety of CDK4/6-dependent tumorigenic cell lines including breast, melanoma, leukemia, and lymphoma cells with EC50 concentrations as low as 23 nM.