A multi-targeted receptor tyrosine kinase inhibitor
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Toceranib

Item No. 17714

Technical Information
Formal Name
5-[(Z)-(5-fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidene)methyl]-2,4-dimethyl-N-[2-(1-pyrrolidinyl)ethyl]-1H-pyrrole-3-carboxamide
CAS Number
356068-94-5
Synonyms
  • PHA 291639
  • SU11654
Molecular Formula
C22H25FN4O2
Formula Weight
Purity
≥95%
A crystalline solid
DMF: 0.25 mg/mlDMSO: 0.5 mg/ml
λmax
267, 430 nm
SMILES
FC1=CC=C(NC(/C2=C\C3=C(C)C(C(NCCN4CCCC4)=O)=C(C)N3)=O)C2=C1
InChi Code
InChI=1S/C22H25FN4O2/c1-13-19(12-17-16-11-15(23)5-6-18(16)26-21(17)28)25-14(2)20(13)22(29)24-7-10-27-8-3-4-9-27/h5-6,11-12,25H,3-4,7-10H2,1-2H3,(H,24,29)(H,26,28)/b17-12-
InChi Key
SRSGVKWWVXWSJT-ATVHPVEESA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    Toceranib is a small molecule, multi-targeted receptor tyrosine kinase inhibitor that is structurally related to sunitinib (Item No. 13159).1 It potently inhibits signaling through VEGFR, FGFR, PDGFR, and Kit.1 Moveover, toceranib blocks the autophosphorylation of both wild type and mutant forms of Kit in response to stem cell factor, resulting in cell death.1 It is active in vivo and is commonly used against solid tumors in dogs.2,3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Liao, A.T., Chien, M.B., Shenoy, N., et alInhibition of constitutively active forms of mutant kit by multitargeted indolinone tyrosine kinase inhibitors. Blood 100(2), 585-593 (2002).

    2. London, C., Mathie, T., Stingle, N., et alPreliminary evidence for biologic activity of toceranib phosphate (Palladiar) in solid tumours. Vet. Comp. Oncol. 10(3), 194-205 (2012).

    3. Ranieri, G., Gadaleta, C.D., Patruno, R., et alA model of study for human cancer: Spontaneous occurring tumors in dogs. Biological features and translation for new anticancer therapies. Crit. Rev. Oncol. Hematol. 88, 187-197 (2013).