PI3K/VEGFR2-IN-1

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Data Sheet Handling Instructions

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PI3K/VEGFR2-IN-1 is a potent dual PI3K/VEGFR2 inhibitor with IC₅₀ values of 2.21 and 68 μM for PI3K and VEGFR2, respectively. PI3K/VEGFR2-IN-1 induces apoptosis. PI3K/VEGFR2-IN-1 can be used in research of cancer.

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

PI3K/VEGFR2-IN-1 Chemical Structure

CAS No. : 2851067-08-6

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PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

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VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

PI3K

2.21 μM (IC₅₀)

VEGFR2

68 μM (IC₅₀)

In Vitro

PI3K/VEGFR2-IN-1 (compound 8; 1.56-100 µM; 24 h; HePG2, MCF-7, Hela, and PC3 cells) inhibits cell proliferative in a dose-dependent manner^[1].
PI3K/VEGFR2-IN-1 (10 mg/mL; 24 h; MCF-7 and Hela cells) arrests cell cycle at G1/S phase and induces apoptosis^[1].

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

Cell Viability Assay^[1]

Cell Line:	HePG2, MCF-7, Hela, and PC3 cells
Concentration:	1.56-100 µM
Incubation Time:	24 hours
Result:	Had antitumor activity with IC₅₀ values of 7.94, 9.73 , 11.58, and 17.49 µM for Hela, HePG2, MCF-7 and PC3 cells, respectively.

Cell Cycle Analysis^[1]

Cell Line:	MCF-7 cells
Concentration:	10 mg/mL
Incubation Time:	24 hours
Result:	Arrested cell cycle in G1/S phase at 24 h by 51.23%.

Cell Cycle Analysis^[1]

Cell Line:	MCF-7 and Hela cells
Concentration:	10 mg/mL
Incubation Time:	24 hours
Result:	Enhanced late apoptotic induction with 14.11% at Hela cells.

Molecular Weight

343.83

Formula

C₁₇H₁₄ClN₃OS

CAS No.

2851067-08-6

SMILES

S=C(N/N=C(C1=CC2=CC=CC=C2O1)\C)NC3=CC=C(Cl)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

Handling Instructions (2659 KB)

References

[1]. El-Khouly OA, et, al. Design, synthesis and computational study of new benzofuran hybrids as dual PI3K/VEGFR2 inhibitors targeting cancer. Sci Rep. 2022 Oct 12;12(1):17104. [Content Brief]

PI3K/VEGFR2-IN-1 Related Classifications

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This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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.

Keywords:

PI3K/VEGFR2-IN-12851067-08-6PI3KVEGFRApoptosisPhosphoinositide 3-kinaseVascular endothelial growth factor receptoranticancercell proliferativeHelaMCF-7cell cycleG1/S phaseInhibitorinhibitorinhibit

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