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

Allitinib tosylate (Synonyms: AST-1306 (TsOH))

Cat. No.: HY-13427 Purity: 99.23%
Handling Instructions

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

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

Allitinib tosylate Chemical Structure

Allitinib tosylate Chemical Structure

CAS No. : 1050500-29-2

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 246 In-stock
Estimated Time of Arrival: December 31
5 mg USD 180 In-stock
Estimated Time of Arrival: December 31
10 mg USD 288 In-stock
Estimated Time of Arrival: December 31
50 mg USD 960 In-stock
Estimated Time of Arrival: December 31
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Description

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

IC50 & Target[1]

EGFR

0.5 nM (IC50)

ErbB2

3 nM (IC50)

EGFRL858R/T790M

12 nM (IC50)

ErbB4

0.8 nM (IC50)

In Vitro

AST1306 tosylate (AST-1306 (TsOH); 0.19-6.25 μM; 72 hours) induces a significant, concentration-dependent inhibition of the growth of HIH3T3-EGFR T790M/L858R cells[1].
AST1306 tosylate inhibits the activation of tyrosine kinases and downstream signaling pathways in A549 cells, Calu-3 cells and SK-OV-3 cells. AST1306 tosylate dose-dependently and markedly inhibits EGF-induced EGFR phosphorylation in A549 cells[1].
AST1306 tosylate (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 tosylate (0.001-1.0 μM; 4 hours) is more than 3000-fold selective for ErbB family kinases over other kinase families[1].
AST1306 tosylate potently inhibits the EGFR T790M/L858R double mutant, exhibiting an IC50 value of 12±2 nmol/L[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 tosylate (AST-1306 (TsOH); 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

621.08

Formula

C₃₁H₂₆ClFN₄O₅S

CAS No.

1050500-29-2

SMILES

FC1=CC=CC(COC2=C(Cl)C=C(NC3=NC=NC4=C3C=C(NC(C=C)=O)C=C4)C=C2)=C1.O=S(C5=CC=C(C)C=C5)(O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (80.50 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6101 mL 8.0505 mL 16.1010 mL
5 mM 0.3220 mL 1.6101 mL 3.2202 mL
10 mM 0.1610 mL 0.8050 mL 1.6101 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (4.03 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.03 mM); Precipitated solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

AllitinibAST-1306 (TsOH)EGFREpidermal growth factor receptorErbB-1HER1Irreversibleanilino-quinazolineanti-cancerInhibitorinhibitorinhibit

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Allitinib tosylate
Cat. No.:
HY-13427
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