A multi-targeted RTK inhibitor
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Amuvatinib

Item No. 21461

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-(1,3-benzodioxol-5-ylmethyl)-4-benzofuro[3,2-d]pyrimidin-4-yl-1-piperazinecarbothioamide
CAS Number
850879-09-3
Synonyms
  • HPK56
  • MP470
Molecular Formula
C23H21N5O3S
Formula Weight
447.5
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mlDMF:PBS (pH 7.2)(1:3): 0.25 mg/mlDMSO: 10 mg/ml
λmax
244, 290, 315 nm
SMILES
S=C(N([H])CC1=CC=C(OCO2)C2=C1)N(CC3)CCN3C4=NC=NC5=C4OC6=C5C=CC=C6
InChi Code
InChI=1S/C23H21N5O3S/c32-23(24-12-15-5-6-18-19(11-15)30-14-29-18)28-9-7-27(8-10-28)22-21-20(25-13-26-22)16-3-1-2-4-17(16)31-21/h1-6,11,13H,7-10,12,14H2,(H,24,32)
InChi Key
FOFDIMHVKGYHRU-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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    5 mg

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    Product Description

    Amuvatinib is a multi-targeted inhibitor of receptor tyrosine kinases that inhibits c-Kit, platelet-derived growth factor receptor α (PDGFRα), and c-Met (IC50s = 10, 40, and 81 nM, respectively).1 It inhibits growth and induces apoptosis in prostate cancer cell lines, with additive effects achieved when combined with erlotinib (Item No. 10483).1 Amuvatinib sensitizes cancer cells to radiation and chemotherapeutic compounds, in part by inhibiting homologous recombination.2,3,4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Qi, W., Cooke, L.S., Stejskal, A., et al. MP470, a novel receptor tyrosine kinase inhibitor, in combination with erlotinib inhibits the HER family/PI3K/Akt pathway and tumor growth in prostate cancer. BMC Cancer 9(142), 1-12 (2009).

    2. Padda, S., Neal, J.W., and Wakelee, H.A. MET inhibitors in combination with other therapies in non-small cell lung cancer. Transl. Lung Cancer Res. 1(4), 238-253 (2012).

    3. Welsh, J.W., Mahadevan, D., Ellsworth, R., et al. The c-Metreceptortyrosine kinaseinhibitor MP470 radiosensitizes glioblastomacells. Radiat. Oncol. 4(69), (2009).

    4. Zhao, H., Luoto, K.R., Meng, A.X., et al. The receptor tyrosine kinase inhibitor amuvatinib (MP470) sensitizes tumor cells to radio- and chemo-therapies in part by inhibiting homologous recombination. Radiother. Oncol. 101(1), 59-65 (2011).