Toceranib - CAS 356068-94-5
Catalog number: B0084-455463
Category: Inhibitor
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Molecular Formula:
C22H25FN4O2
Molecular Weight:
396.46
COA:
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Targets:
PDGFR | VEGFR
Description:
Toceranib (CAS 356068-94-5) is a potent ATP-competitive PDGFR and VEGFR inhibitor (Ki = 5 and 6 nM, respectively); inhibits phosphorylation of c-Kit and suppresses the growth of mast cell lines expressing mutant Kit, inducing cell cycle arrest and apoptosis. Also inhibits FGFR1 (Ki = 0.5 μM). Effective in vivo.
Purity:
>98%
Synonyms:
SU 11654; PHA 291639; SU11654; SU-11654; PHA-291639; PHA291639
MSDS:
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InChIKey:
SRSGVKWWVXWSJT-ATVHPVEESA-N
InChI:
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-
Canonical SMILES:
CC1=C(NC(=C1C(=O)NCCN2CCCC2)C)C=C3C4=C(C=CC(=C4)F)NC3=O
1.Retrospective evaluation of toceranib phosphate (Palladia) in cats with oral squamous cell carcinoma.
Wiles V1, Hohenhaus A2, Lamb K3, Zaidi B2, Camps-Palau M2, Leibman N2. J Feline Med Surg. 2016 Jan 11. pii: 1098612X15622237. [Epub ahead of print]
OBJECTIVES: The aim of the study was to determine the clinical benefit and adverse event profile of toceranib phosphate in the treatment of feline oral squamous cell carcinoma (FOSCC).
2.Retrospective evaluation of toceranib phosphate (Palladia®) toxicity in cats.
Merrick CH1, Pierro J2, Schleis SE3, Sones EA4, Wright ZM5, Regan RC6, Siedlecki CT1, Bergman PJ7. Vet Comp Oncol. 2016 Apr 4. doi: 10.1111/vco.12211. [Epub ahead of print]
The purpose of this study was to describe the toxicity profile of toceranib phosphate in tumour bearing cats. Medical records were reviewed from seven institutions. Patients with incomplete medical records and those receiving concurrent chemotherapy or NSAIDs (non-steroidal anti-inflammatory) were excluded. Fifty-five cats met the inclusion criteria. Carcinoma was diagnosed in 55% of cases. Median oral toceranib dose was 2.7 mg kg-1 and was most commonly administered on Monday, Wednesday and Friday. Thrombocytopenia (16.3%) and neutropenia (9.1%) were the most common haematologic toxicities. Azotemia (14.5%) and alanine aminotransferase (ALT) elevations (7.2%) were the most frequently encountered biochemical alterations. Gastrointestinal (GI) toxicity was seen in 21.8% of cats, and was lower than previously reported in dogs. The results of this study showed that treatment of cats with toceranib is well-tolerated and toxicity is uncommon.
3.Phase 1 Dose-Escalation Study with LEC/chTNT-3 and Toceranib Phosphate (Palladia®) in Dogs with Spontaneous Malignancies.
Jang JK1, Chretin J2, Bruyette D2, Hu P1, Epstein AL1. J Cancer Sci Ther. 2015;7(6):167-174. Epub 2015 May 30.
OBJECTIVES: LEC chemokine promotes TH1 responses and recruits immune cells to inflammatory sites. By linking LEC to an antibody targeting tumor necrosis, LEC/chTNT-3 can be used for the immunotherapeutic treatment of tumors. The primary objective of this study was to determine the safety profile of LEC/chTNT-3 and toceranib phosphate (Palladia®) combination therapy in dogs with spontaneous malignancies. Secondary purpose was to determine objective responses to treatment.
4.Pulse-Administered Toceranib Phosphate Plus Lomustine for Treatment of Unresectable Mast Cell Tumors in Dogs.
Burton JH1,2, Venable RO1,3, Vail DM4, Williams LE5,6, Clifford CA7,8, Axiak-Bechtel SM9, Avery AC10, Thamm DH1. J Vet Intern Med. 2015 Jul-Aug;29(4):1098-104. doi: 10.1111/jvim.13573. Epub 2015 Jun 25.
BACKGROUND: Nonresectable mast cell tumors (MCT) in dogs remain a therapeutic challenge, and investigation of novel combination therapies is warranted. Intermittent administration of tyrosine kinase inhibitors (TKI) combined with cytotoxic chemotherapy may effectively chemosensitize canine MCT while decreasing cost and adverse effects associated with either agent administered as monotherapy.
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CAS 356068-94-5 Toceranib

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