1. Protein Tyrosine Kinase/RTK Cell Cycle/DNA Damage JAK/STAT Signaling Apoptosis
  2. VEGFR CDK EGFR Necroptosis Apoptosis
  3. Multi-kinase-IN-4

Multi-kinase-IN-4 (compound 5d) is multi-targeted kinase inhibitor, including VEGFR2, EGFR, HER2, and CDK2, with IC50 values of 0.33, 0.22, 0.18 and 2.09 μM, respectively. Multi-kinase-IN-4 shows broad-spectrum anti-cancer activities against HepG2, MCF-7, MDA-231, and HeLa cell lines (IC50 = 1.94–7.1 µM), but exhibits lower toxicity in the WI-38 cells (IC50 = 40.85 µM). Multi-kinase-IN-4 induces apoptosis and arrests cell cycle at S phase in HepG2 cells. Multi-kinase-IN-4 has the potential for the research of cancer.

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Multi-kinase-IN-4 Chemical Structure

Multi-kinase-IN-4 Chemical Structure

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Description

Multi-kinase-IN-4 (compound 5d) is multi-targeted kinase inhibitor, including VEGFR2, EGFR, HER2, and CDK2, with IC50 values of 0.33, 0.22, 0.18 and 2.09 μM, respectively. Multi-kinase-IN-4 shows broad-spectrum anti-cancer activities against HepG2, MCF-7, MDA-231, and HeLa cell lines (IC50 = 1.94–7.1 µM), but exhibits lower toxicity in the WI-38 cells (IC50 = 40.85 µM). Multi-kinase-IN-4 induces apoptosis and arrests cell cycle at S phase in HepG2 cells. Multi-kinase-IN-4 has the potential for the research of cancer[1].

IC50 & Target

VEGFR2

0.33 μM (IC50)

CDK2

2.09 μM (IC50)

HER2

0.18 mM (IC50)

In Vitro

Multi-kinase-IN-4 (compound 5d) (48 h) has cytotoxic against the HepG2, MCF-7, MDA-231, and HeLa cell lines with IC50 values of 7.10, 2.48, 1.94, and 6.38 µM, respectively, but displays less cytotoxic activity on the WI38 cells (IC50 = 64.29 µM) [1].
Multi-kinase-IN-4 (7.1 µM, 24 h, HepG2 cells ) increases the cell population of 9.23% at the S phase and results in a drop in the cell population at the G0-G1 and G2/M phases: 4.50% and 4.73%, respectively[1].
Multi-kinase-IN-4 (7.1 µM, 24 h, HepG2 cells) induces early and late apoptosis as well as necrotic cell death by 7.51%, 3.45%, and 3.08%, respectively[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Apoptosis Analysis[1]

Cell Line: HepG2
Concentration: 7.1 µM
Incubation Time: 24h
Result: Induced early and late apoptosis as well as necrotic cell death by 7.51%, 3.45%, and 3.08%, respectively.

Cell Cycle Analysis[1]

Cell Line: HepG2
Concentration: 7.1 µM
Incubation Time: 24h
Result: Increased the cell population of 9.23% at the S phase and results in a drop in the cell population at the G0-G1 and G2/M phases: 4.50% and 4.73%, respectively
Molecular Weight

402.91

Formula

C21H20ClFN2OS

SMILES

O=C1N(C/C=C(CC)\C)C(SCC2=CC=C(Cl)C=C2)=NC3=C1C=C(F)C=C3

Shipping

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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  • 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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Multi-kinase-IN-4
Cat. No.:
HY-149407
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