An irreversible inhibitor of EGFR, HER2, and HER4
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AST-1306 (tosylate)

Item No. 29708

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[4-[[3-chloro-4-[(3-fluorophenyl)methoxy]phenyl]amino]-6-quinazolinyl]-2-propenamide, 4-methylbenzenesulfonate
CAS Number
1050500-29-2
Synonyms
  • Allitinib
Molecular Formula
C24H18ClFN4O2 • C7H8O3S
Formula Weight
621.1
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 25 mg/mlDMF:PBS (pH 7.2) (1:3): 0.25 mg/mlDMSO: 20 mg/mlEthanol: 1 mg/ml
λmax
252, 307, 367 nm
SMILES
O=C(C=C)NC(C=C1)=CC2=C1N=CN=C2NC3=CC(Cl)=C(OCC4=CC(F)=CC=C4)C=C3.CC5=CC=C(S(O)(=O)=O)C=C5
InChi Code
InChI=1S/C24H18ClFN4O2.C7H8O3S/c1-2-23(31)29-17-6-8-21-19(11-17)24(28-14-27-21)30-18-7-9-22(20(25)12-18)32-13-15-4-3-5-16(26)10-15;1-6-2-4-7(5-3-6)11(8,9)10/h2-12,14H,1,13H2,(H,29,31)(H,27,28,30);2-5H,1H3,(H,8,9,10)
InChi Key
ZMUKJEHWLJBODV-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    10 mg

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    25 mg

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    Product Description

    AST-1306 is an irreversible inhibitor of EGFR, HER2, and HER4 (IC50s = 0.5, 3, and 0.8 nM, respectively).1 It is selective for EGFR, HER2, and HER4 over a panel of 23 additional kinases (IC50s = >10 µM). AST-1306 also inhibits EGFRT790M/L858R with an IC50 value of 12 nM in a cell-free assay. It decreases EGFR, ERK1/2, and Akt phosphorylation in Calu-3, A549, and SKOV3 cancer cells when used at concentrations ranging from 0.001 to 1 µM. AST-1306 inhibits proliferation of Calu-3, BT474, MDA-MB-468, A549, SKOV3, NCI H23, and MCF-7 cells (IC50s = 0.23-16 µM). It reduces tumor growth in Calu-3, A549, SKOV3, and HO8910 mouse xenograft models when administered at doses of 25, 50, and 100 mg/kg per day.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. 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 6(7), e21487 (2011).