1. Protein Tyrosine Kinase/RTK
    JAK/STAT Signaling
  2. EGFR
  3. Allitinib

Allitinib (Synonyms: AST-1306; ALS 1306)

Cat. No.: HY-15375
Handling Instructions

Allitinib (AST-1306) is an orally active and irreversible EGFR and ErbB2 inhibitor with IC50s of 0.5 and 3 nM, respectively. Allitinib also inhibits ErbB4 with an IC50 of 0.8 nM. Allitinib is an anilino-quinazoline compound and has anti-cancer activity.

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Allitinib Chemical Structure

Allitinib Chemical Structure

CAS No. : 897383-62-9

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Description

Allitinib (AST-1306) is an orally active and irreversible EGFR and ErbB2 inhibitor with IC50s of 0.5 and 3 nM, respectively. Allitinib also inhibits ErbB4 with an IC50 of 0.8 nM. Allitinib is an anilino-quinazoline compound and has anti-cancer activity[1].

IC50 & Target[1]

EGFR

0.5 nM (IC50)

EGFRL858R/T790M

12 nM (IC50)

ErbB2

3 nM (IC50)

ErbB4

0.8 nM (IC50)

In Vitro

AST1306 (AST-1306; 0.19-6.25 μM; 72 hours) induces a significant, concentration-dependent inhibition of the growth of HIH3T3-EGFR T790M/L858R cells[1].
AST1306 inhibits the activation of tyrosine kinases and downstream signaling pathways in A549 cells, Calu-3 cells and SK-OV-3 cells. AST1306 dose-dependently and markedly inhibits EGF-induced EGFR phosphorylation in A549 cells[1].
AST1306 (0.1, 0.5, 1.0, 5.0 μM) can dramatically inhibit the growth of both tumor cells on soft agar, and SK-OV-3 cells exhibited much more sensitivity than that of A549 cells[1].
AST1306 (0.001-1.0 μM; 4 hours) is more than 3000-fold selective for ErbB family kinases over other kinase families[1].
AST1306 potently inhibits the EGFR T790M/L858R double mutant, exhibiting an IC50 value of 12 nM[1].

Cell Proliferation Assay[1]

Cell Line: NIH3T3 parental cells and NIH3T3 cells
Concentration: 0.19, 0.39, 0.78, 1.56, 3.13, 6.25 μM
Incubation Time: 72 hours
Result: Induced a significant, concentration-dependent inhibition of the growth of HIH3T3-EGFR T790M/L858R cells.

Western Blot Analysis[1]

Cell Line: A549 cells , Calu-3 cells and SK-OV-3 cells
Concentration: 0.001, 0.01, 0.1, 1.0 μM
Incubation Time: 4 hours
Result: Inhibits the activation of tyrosine kinases and downstream signaling pathways.
In Vivo

AST1306 (AST-1306; p.o.; 25-100 mg/kg; twice daily; for 28 days) causes a dramatic suppression of tumor growth in SK-OV-3 and Calu-3 xenograft models[1].

Animal Model: Nude mice with SK-OV-3 and Calu-3 tumors[1]
Dosage: 25, 50, 100 mg/kg
Administration: p.o; twice daily; for 28 days
Result: Caused a dramatic suppression of tumor growth.
Molecular Weight

448.88

Formula

C₂₄H₁₈ClFN₄O₂

CAS No.

897383-62-9

SMILES

FC1=CC=CC(COC2=C(Cl)C=C(NC3=NC=NC4=C3C=C(NC(C=C)=O)C=C4)C=C2)=C1

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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.

References
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Keywords:

AllitinibAST-1306ALS 1306AST1306AST 1306ALS1306ALS-1306EGFREpidermal growth factor receptorErbB-1HER1Irreversibleanilino-quinazolineanti-cancerInhibitorinhibitorinhibit

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