Toceranib Phosphate

SKU: orb1299858

Description

Toceranib phosphate (SU11654 phosphate) is a selective tyrosine kinase inhibitor targeting receptors such as Flk-1/KDR and PDGFR. It has been utilized in preclinical in vitro and in vivo studies within oncology research, particularly for investigating angiogenesis and tumor cell proliferation.

Research Area

Cardiovascular Research, Protein Biochemistry, Signal Transduction

Key Properties

• CAS Number: 874819-74-6
• MW: 494.45
• Purity: 98.56% (May vary between batches)
• Formula: C₂₂H₂₈FN₄O₆P
• SMILES: OP(O)(O)=O.Cc1[nH]c(\C=C2/C(=O)Nc3ccc(F)cc23)c(C)c1C(=O)NCCN1CCCC1
• Target: Tyrosinase,VEGFR,PDGFR,c-Kit
• Solubility: DMSO:Slightly soluble

Bioactivity

• Target IC50:
  PDGFRβ:5 nM (Ki)|FLK1:6 nM (Ki)
• In Vivo:
  Systolic blood pressure was significantly (P = 0.0013) higher in previously normotensive treatment dogs after initiation of treatment with toceranib phosphate (152 mmHg ± 19) compared to baseline (136 mmHg ± 14). 37% of treated dogs developed SBP ≥ 160 mmHg. The prevalence of systemic hypertension (37%) and proteinuria (21%) at baseline in treatment dogs did not differ from that of age-matched healthy controls (15% [P = 0.13] and 0% [P = 0.069], respectively).
• Animal Research:
  Dogs scheduled to received toceranib phosphate treatment were divided into 2 groups based on SBP recorded at screening: dogs that were normotensive were assigned to Group 2a and dogs diagnosed with HT were assigned to Group 2b. After baseline evaluation, dogs enrolled in Group 2a received toceranib phosphate at a standard dose as previously published.2 Group 2b dogs received toceranib phosphate as described, but were also treated with standard‐of‐care treatment for HT, including amlodipine besylate (0.2–0.4 mg/kg PO q 24 hours), enalapril maleate (0.5 mg/kg PO q 12 hours), or both, initiated at the discretion of the attending veterinarian. Some dogs were treated with additional medications, including corticosteroids, at the discretion of the oncologist. All dogs were re‐evaluated on Day 14 (±3 days) at which time a UPC and blood pressure measurements were performed.

Storage & Handling

• Storage: store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Toceranib Phosphate, Toceranib, PHA 291639E, PHA 291639 Phosphate, PHA291639 Phosphate, PHA-291639 Phosphate, PHA 291639 phosphate, SCFR, SU 11654 Phosphate, SU 11654, SU11654 Phosphate, SU11654 phosphate, SU-11654 Phosphate, SU-11654, SU11654, tyrosine kinase, VEGFR, Vascular endothelial growth factor receptor, CD117, cKit, c-Kit, inhibit, PDGFR, Platelet-derived growth factor receptor, Inhibitor

Compound Identifiers

PubChem CID

16034840