SHP2/CDK4-IN-1

SHP2/CDK4-IN-1 (compound 10) is an orally active and potent SHP2 and CDK4 dual inhibitor, with IC50 values of 4.3 and 18.2 nM, respectively. SHP2/CDK4-IN-1 effectively induces G0/G1 arrest to prevent the proliferation of TNBC cell lines. SHP2/CDK4-IN-1 shows significant antitumor efficacy in the EMT6 syngeneic mouse model. SHP2/CDK4-IN-1 can be used for triple-negative breast cancer (TNBC) research[1].

Product Specifications

CAS Number

[2924036-87-1]

UNSPSC

12352005

Target

CDK; Phosphatase; SHP2

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage; Metabolic Enzyme/Protease; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/shp2-cdk4-in-1.html

Solubility

10 mM in DMSO

Smiles

CC(C)N1C(C)=NC2=C(C=C(C=C12)C3=NC(NC4=C(C(SC5=NC=C(N=C5)N6CCC7([C@H](N)[C@H](C)OC7)CC6)=CC=N4)Cl)=NC=C3F)F

Molecular Formula

C33H35ClF2N10OS

Molecular Weight

693.21

References & Citations

[1]Chen X, et al. Discovery of a Novel Src Homology-2 Domain Containing Protein Tyrosine Phosphatase-2 (SHP2) and Cyclin-Dependent Kinase 4 (CDK4) Dual Inhibitor for the Treatment of Triple-Negative Breast Cancer. J Med Chem. 2022 May 12;65 (9) :6729-6747.