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Allitinib tosylate

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Allitinib tosylate
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Cat #: V34046 CAS #: 1050500-29-2 Purity ≥ 99%

Description: Allitinib tosylate (formerly AST-1306; AST1306; AST 1306), the tosylate of Allitinib, is a selective and covalent/irreversible inhibitor of EGFR and ErbB2 with potential anticancer activity.

References: Xie H, Lin L, Tong L et al. AST1306, a novel irreversible inhibitor of the epidermal growth factor receptor 1 and 2, exhibits antitumor activity both in vitro and in vivo. PLoS One. 2011;6(7):e21487.

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Molecular Weight (MW)621.08
Molecular FormulaC31H26ClFN4O5S
CAS No.1050500-29-2
SMILES CodeC=CC(NC1=CC2=C(NC3=CC=C(OCC4=CC=CC(F)=C4)C(Cl)=C3)N=CN=C2C=C1)=O.OS(=O)(C5=CC=C(C)C=C5)=O
Synonyms Allitinib tosylate; AST1306 TsOH; AST-1306 TsOH; AST 1306 TsOH; ALS1306 TsOH; ALS-1306 TsOH; ALS1306 TsOH; AST 6 TsOH; AST-6 TsOH; AST6 TsOH
ProtocolIn VitroAST1306 tosylate potently inhibits the EGFR T790M/L858R double mutant, exhibiting an IC50 value of 12±2 nmol/L. AST1306 tosylate (0.001-1.0 μM; 4 hours) is more than 3000-fold selective for ErbB family kinases over other kinase families. 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. 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. 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.
In VivoAST1306 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.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Preparing Stock Solutions
Solvent volume to be added Mass (the weight of a compound)
Mother liquor concentration 1mg5mg10mg20mg
1mM1.6101 mL8.0505 mL16.1010 mL32.2020 mL
5mM0.3220 mL1.6101 mL3.2202 mL6.4404 mL
10mM0.1610 mL0.8050 mL1.6101 mL3.2202 mL
20mM0.0805 mL0.4025 mL0.8050 mL1.6101 mL
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
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The dilution calculator equation
Concentration(start) × Volume(start) = Concentration(final) × Volume(final)

This equation is commonly abbreviated as: C1 V1 = C2 V2

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Step One: Enter information below
Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals
Step Two: Enter the in vivo formulation
%DMSO + % + %Tween 80 + %ddH2O

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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in µL DMSO(Master liquid concentration mg/mL) ,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation: Take µL DMSO master liquid, next add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH2O,mix and clarify.
Note:
  • (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
  • (2) Be sure to add the solvent(s) in order.