A VEGFR2 inhibitor
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XL184

Item No. 18464

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N'-[4-[(6,7-dimethoxy-4-quinolinyl)oxy]phenyl]-N-(4-fluorophenyl)-1,1-cyclopropanedicarboxamide
CAS Number
849217-68-1
Synonyms
  • BMS-907351
  • Cabozantinib
Molecular Formula
C28H24FN3O5
Formula Weight
501.5
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 3 mg/mlDMSO: 5 mg/mlDMSO:PBS(pH 7.2) (1:2): 0.3 mg/mlEthanol: 2 mg/ml
λmax
242, 308, 322 nm
SMILES
COC1=C(OC)C=C(C(OC2=CC=C(NC(C3(C(NC4=CC=C(F)C=C4)=O)CC3)=O)C=C2)=CC=N5)C5=C1
InChi Code
InChI=1S/C28H24FN3O5/c1-35-24-15-21-22(16-25(24)36-2)30-14-11-23(21)37-20-9-7-19(8-10-20)32-27(34)28(12-13-28)26(33)31-18-5-3-17(29)4-6-18/h3-11,14-16H,12-13H2,1-2H3,(H,31,33)(H,32,34)
InChi Key
ONIQOQHATWINJY-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $49

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    5 mg

    $107

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    10 mg

    $167

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    50 mg

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    Product Description

    XL184 is an inhibitor of VEGFR2 (IC50 = 0.035 nM).1 It is selective for VEGFR2 over Ron, EGFR, IGF-1R, and EphA4/B4, but also inhibits c-Met, RET, c-Kit, Axl, FLT3, and Tie2 (IC50s = 1.3, 5.2, 4.6, 7, 11.3, and 14.3 nM, respectively). XL184 (4.6 nM) inhibits VEGF-induced tubule formation in human microvascular endothelial cells (HMVECs). It reduces migration and invasion of B16/F10 melanoma cells induced by hepatocyte growth factor (HGF) when used at a concentration of 123 nM. XL184 (60 mg/kg) induces tumor regression in an MDA-MB-231 breast cancer mouse xenograft model. Unlike sunitinib (Item No. 13159), XL184 does not increase the number of pulmonary tumor foci in an MDA-MB-231 mouse metastasis model. It also protects primary placental fibroblasts from Zika virus infection.2 Formulations containing XL184 have been used in the treatment of renal cell and hepatocellular carcinomas.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Yakes, F.M., Chen, J., Tan, J., et al. Cabozantinib (XL184), a novel MET and VEGFR2 inhibitor, simultaneously suppresses metastasis, angiogenesis, and tumor growth. Mol. Cancer Ther. 10(12), 2298-2308 (2011).

    2. Rausch, K., Hackett, B., Weinbren, N.R., S., et al. Screening bioactives reveals nanchangmycin as a broad spectrum antiviral active against Zika virus. Cell Rep. 18(3), 804-815 (2017).