A dual inhibitor of EGFR and HER2
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AC480

Item No. 29657

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[4-[[1-[(3-fluorophenyl)methyl]-1H-indazol-5-yl]amino]-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl]-carbamic acid, (3S)-3-morpholinylmethyl ester
CAS Number
714971-09-2
Synonyms
  • BMS-599626
Molecular Formula
C27H27FN8O3
Formula Weight
530.6
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mlDMSO: 16 mg/mlEthanol: 0.3 mg/ml
λmax
254, 312 nm
SMILES
CC(C(NC(OC[C@H]1NCCOC1)=O)=C2)=C3N2N=CN=C3NC4=CC=C5C(C=NN5CC6=CC(F)=CC=C6)=C4
InChi Code
InChI=1S/C27H27FN8O3/c1-17-23(34-27(37)39-15-22-14-38-8-7-29-22)13-36-25(17)26(30-16-32-36)33-21-5-6-24-19(10-21)11-31-35(24)12-18-3-2-4-20(28)9-18/h2-6,9-11,13,16,22,29H,7-8,12,14-15H2,1H3,(H,34,37)(H,30,32,33)/t22-/m0/s1
InChi Key
LUJZZYWHBDHDQX-QFIPXVFZSA-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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    Product Description

    AC480 is a dual inhibitor of EGFR and HER2 (IC50s = 22 and 32 nM, respectively).1 It is selective for EGFR and HER2 over HER4 (IC50 = 190 nM) and a panel of 21 additional kinases (IC50s = >2,500 nM for all). AC480 inhibits proliferation in a panel of EGFR and/or HER2 signaling-dependent cancer cells (IC50s = 0.24-0.94 μM). It reduces tumor growth in a Sal2 murine salivary gland tumor model, as well as GEO colon and KPL4 breast cancer mouse xenograft models in a dose-dependent manner. AC480 (100 mg/kg) reduces tumor cell motility, intravasation, and EGF-induced invasion in an MTLn3E metastatic mammary adenocarcinoma mouse xenograft model.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Wong, T.W., Lee, F.Y., Yu, C., et al. Preclinical antitumor activity of BMS-599626, a pan-HER kinase inhibitor that inhibits HER1/HER2 homodimer and heterodimer signaling. Clin. Cancer Res. 12(20 Pt 1), 6186-6193 (2006).

    2. Kedrin, D., Wyckoff, J., Boimel, P., et al. ERBB1 and ERBB2 have distinct functions in tumor cell invasion and intravasation. Clin. Cancer Res. 15(11), 3733-3739 (2009).