A multiple kinase inhibitor
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Altiratinib

Item No. 18777

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[4-[[2-[(cyclopropylcarbonyl)amino]-4-pyridinyl]oxy]-2,5-difluorophenyl]-N'-(4-fluorophenyl)-1,1-cyclopropanedicarboxamide
CAS Number
1345847-93-9
Molecular Formula
C26H21F3N4O4
Formula Weight
510.5
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 10 mg/mlDMSO: 10 mg/mlDMSO:PBS(pH 7.2) (1:2): 0.25 mg/ml
λmax
243 nm
SMILES
FC1=CC=C(NC(C2(CC2)C(NC3=C(F)C=C(OC4=CC(NC(C5CC5)=O)=NC=C4)C=C3F)=O)=O)C=C1
InChi Code
InChI=1S/C26H21F3N4O4/c27-15-3-5-16(6-4-15)31-24(35)26(8-9-26)25(36)33-22-19(28)11-18(12-20(22)29)37-17-7-10-30-21(13-17)32-23(34)14-1-2-14/h3-7,10-14H,1-2,8-9H2,(H,31,35)(H,33,36)(H,30,32,34)
InChi Key
PNQGOEOAPBQVPV-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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    Product Description

    Altiratinib is a multiple kinase inhibitor, blocking Met, Tie2, VEGF2, TrkA, TrkB, and TrkC with IC50 values of 2.7, 8.0, 9.2, 0.85, 4.6, and 0.83 nM, respectively.1 It also inhibits several mutant Met isoforms at nanomolar concentrations. Altiratinib inhibits the proliferation of several cancer cell lines in vitro and blocks capillary tube formation by HMVEC cells.1 It is orally bioavailable and penetrates the blood brain barrier, suppressing the growth of subcutaneous and intracerebroventricular xenograft tumors in mice.1,2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Smith, B.D., Kaufman, M.D., Leary, C.B., et al. Altiratinib Inhibits Tumor Growth, Invasion, Angiogenesis, and Microenvironment-Mediated Drug Resistance via Balanced Inhibition of MET, TIE2, and VEGFR2. Mol. Cancer Ther. 14(9), 2023-2034 (2015).

    2. Piao, Y., Park, S.Y., Henry, V., et al. Novel MET/TIE2/VEGFR2 inhibitor altiratinib inhibits tumor growth and invasiveness in bevacizumab-resistant glioblastoma mouse models. Neuro. Oncol. 18(9), 1230-1241 (2016).