1. Protein Tyrosine Kinase/RTK Metabolic Enzyme/Protease Cell Cycle/DNA Damage
  2. SHP2 Phosphatase CDK
  3. 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.

For research use only. We do not sell to patients.

SHP2/CDK4-IN-1 Chemical Structure

SHP2/CDK4-IN-1 Chemical Structure

CAS No. : 2924036-87-1

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Description

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].

IC50 & Target

CDK4

18.2 ± 1.3 nM (IC50)

Cellular Effect
Cell Line Type Value Description References
EMT6 IC50
0.64 μM
Compound: 10
Antiproliferative activity against mouse EMT6 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
Antiproliferative activity against mouse EMT6 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
[PMID: 35447031]
MDA-MB-231 IC50
5.57 μM
Compound: 10
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
[PMID: 35447031]
MDA-MB-468 IC50
1.76 μM
Compound: 10
Antiproliferative activity against human MDA-MB-468 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
Antiproliferative activity against human MDA-MB-468 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
[PMID: 35447031]
Molecular Weight

693.21

Formula

C33H35ClF2N10OS

CAS No.
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

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
SHP2/CDK4-IN-1
Cat. No.:
HY-150609
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