1. JAK/STAT Signaling Protein Tyrosine Kinase/RTK Stem Cell/Wnt Cell Cycle/DNA Damage Cytoskeleton Apoptosis
  2. EGFR VEGFR Casein Kinase Topoisomerase Microtubule/Tubulin Apoptosis
  3. EGFR-IN-57

EGFR-IN-57 (Compound 25a) is a potent, orally active EGFR-TK inhibitor with an IC50 of 0.054 µM. EGFR-IN-57 also inhibits VEGFR-2, CK2α, topoisomerase IIβ and tubulin polymerization with IC50 values of 0.087, 0.171, 0.13 and 3.61 µM, respectively. EGFR-IN-57 induces cell cycle arrest at G2/M and pre-G1 phases. EGFR-IN-57 induces cancer cell apoptosis.

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EGFR-IN-57 Chemical Structure

EGFR-IN-57 Chemical Structure

CAS No. : 2492382-37-1

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Description

EGFR-IN-57 (Compound 25a) is a potent, orally active EGFR-TK inhibitor with an IC50 of 0.054 µM. EGFR-IN-57 also inhibits VEGFR-2, CK2α, topoisomerase IIβ and tubulin polymerization with IC50 values of 0.087, 0.171, 0.13 and 3.61 µM, respectively. EGFR-IN-57 induces cell cycle arrest at G2/M and pre-G1 phases. EGFR-IN-57 induces cancer cell apoptosis[1].

IC50 & Target

EGFR

0.054 μM (IC50)

VEGFR-2

0.087 μM (IC50)

topoisomerase II beta

0.13 μM (IC50)

CK2α

0.171 μM (IC50)

tubulin polymerization

3.16 μM (IC50)

Molecular Weight

385.44

Formula

C22H15N3O2S

CAS No.
SMILES

O=C1N=C(NC2=NOC(C)=C2)S/C1=C\C3=C4C=CC=CC4=CC5=CC=CC=C35

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Room temperature in continental US; may vary elsewhere.

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

Purity & Documentation
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    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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EGFR-IN-57
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HY-146138
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