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Allitinib (AST 1306)

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Allitinib (AST 1306)
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Size Price Stock
100mg$1020Check With Us
250mg$1690Check With Us
500mg$2535Check With Us

Cat #: V0561 CAS #: 897383-62-9 Purity ≥ 98%

Description: Allitinib (formerly also known as AST1306; AST-1306) is a novel, potent, selective and covalent / irreversible inhibitor of EGFR and ErbB2 with potential antitumor 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)448.88
Molecular FormulaC24H18ClFN4O2
CAS No.897383-62-9
Storage-20℃ for 3 years in powder formr
-80℃ for 2 years in solvent
Solubility In VitroDMSO: 124 mg/mL (199.6 mM)r
Water: <1 mg/mLr
Ethanol: <1 mg/mL
Solubility In Vivo0.5% hydroxyethyl cellulose: 30mg/mL
SMILES CodeC=CC(NC1=CC2=C(NC3=CC=C(OCC4=CC=CC(F)=C4)C(Cl)=C3)N=CN=C2C=C1)=O
SynonymsAllitinib; AST1306; ALS-1306; ALS1306; AST 6; AST-6; AST-1306; Allitinib free base; AST 1306; ALS1306; AST6.
ProtocolIn VitroAST1306 potently inhibits the EGFR T790M/L858R double mutant, exhibiting an IC50 value of 12 nM. AST1306 (0.001-1.0 μM; 4 hours) is more than 3000-fold selective for ErbB family kinases over other kinase families. 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. 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. 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.
In VivoAST1306 (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.
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
1mM2.2278 mL11.1388 mL22.2777 mL44.5553 mL
5mM0.4456 mL2.2278 mL4.4555 mL8.9111 mL
10mM0.2228 mL1.1139 mL2.2278 mL4.4555 mL
20mM0.1114 mL0.5569 mL1.1139 mL2.2278 mL
Quality Control Documentation
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
Mass
=
Concentration
×
Volume
×
Molecular Weight*
The dilution calculator equation
Concentration(start) × Volume(start) = Concentration(final) × Volume(final)

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

Concentration(start)
C1
×
Volume(start)
V1
=
Concentration(final)
C2
×
Volume(final)
V2
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

Calculation Results:
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.