Cabozantinib

SKU: orb1223863

Description

Cabozantinib (XL184, BMS-907351) is a potent multi-kinase inhibitor that inhibits VEGFR2, c-Met, Kit, Axl and Flt3 with IC50 of 0.035, 1.3, 4.6, 7 and 11.3 nM, respectively; eliminates tumor vasculature, reduces pericytes and empty basement membrane sleeves, causes widespread intratumoral hypoxia and tumor cell apoptosis, and slows regrowth of the tumor vasculature, also decreases invasiveness of primary tumors and reduces metastasis in pancreatic islet cancer; exerts marked anti-MPNST effects in vitro and in vivo.Kidney Cancer Approved(In Vitro):Cabozantinib inhibits phosphorylation of MET and VEGFR2, as well as KIT, FLT3, and AXL with IC50 values of 7.8, 1.9, 5.0, 7.5, and 42 μM, respectively.Cabozantinib (4.6 nM) inhibits tubule formation with no evidence of cytotoxicity, with IC50 values of 6.7, 5.1, 4.1, 7.7, and 4.7 nM in HMVEC, MDA-MB-231, A431, HT1080, and B16F10 cells, respectively.Cabozantinib (0-370 nM, 24 h) inhibits cellular migration and invasion.Cabozantinib (48 h) inhibits tumor cell proliferation in a variety of tumor types.(In Vivo):Cabozantinib (100 mg/kg, Orally, once) inhibits MET and VEGFR2 phosphorylation in mice.Cabozantinib (100 mg/kg, Orally, once) significantly increases tumor hypoxia and apoptosis.Cabozantinib (0-60 mg/kg, Orally, once daily for 14 days) inhibits tumor growth in a dose-dependent manner.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 849217-68-1
• MW: 501.5057
• Purity: >98% (HPLC)
• Formula: C₂₈H₂₄FN₃O₅
• SMILES: COC1=CC2=NC=CC(OC3=CC=C(C=C3)N(C(=O)C3(CC3)C(N)=O)C3=CC=C(F)C=C3)=C2C=C1OC
• Target: VEGFR
• Solubility: DMSO: ≥ 30 mg/mL

Bioactivity

• In Vivo:
  Cabozantinib (100 mg/kg, Orally, once) inhibits MET and VEGFR2 phosphorylation in mice. Cabozantinib (100 mg/kg, Orally, once) significantly increases tumor hypoxia and apoptosis. Cabozantinib (0-60 mg/kg, Orally, once daily for 14 days) inhibits tumor growth in a dose-dependent manner. Animal model: Female mice bearing MBA-MB-231 tumor (5 per group). Dosage: 0, 100 mg/kg. Administration: Orally, once. Result: Inhibited MET and VEGFR2 phosphorylation. Animal model: Mice bearing MBA-MB-231 tumor. Dosage: 1, 3, 10, 30, 60 mg/kg. Administration: Orally, once daily for 14 days. Result: Inhibited tumor growth in a dose-dependent manner.
  Read more...
• In Vitro:
  Cabozantinib inhibits phosphorylation of MET and VEGFR2, as well as KIT, FLT3, and AXL with IC50 values of 7.8, 1.9, 5.0, 7.5, and 42 μM, respectively. Cabozantinib (4.6 nM) inhibits tubule formation with no evidence of cytotoxicity, with IC50 values of 6.7, 5.1, 4.1, 7.7, and 4.7 nM in HMVEC, MDA-MB-231, A431, HT1080, and B16F10 cells, respectively. Cabozantinib (0-370 nM, 24 h) inhibits cellular migration and invasion. Cabozantinib (48 h) inhibits tumor cell proliferation in a variety of tumor types. Cell Proliferation Assay Cell line: SNU-5, Hs746T, SNU-1, SNU-16, MDA-MB-231, U87MG, H441, H69, and PC3 cells. Concentration: Incubation time: 48 hours. Result: Inhibited tumor cell proliferation, with IC50 of 19, 9.9, 5223, 1149, 6421, 1851, 21700, 20200, and 10800 nM, respectively. Cell Migration Assay Cell line: B16F10 cells. Concentration: 0, 41, 123, and 370 nM. Incubation time: 24 hours. Result: Potently inhibited HGF-induced migration (IC50 = 31 nM) of B16F10 cells. Cell Invasion Assay Cell line: B16F10 cells. Concentration: 0, 1.5, 14, and 123 nM Incubation time: 24 hours. Result: Potently inhibited HGF-induced invasion (IC50 = 9 nM) of B16F10 cells.
  Read more...

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

XL184 | BMS-907351 | XL-184 | XL184

Quick Database Links

Gene Symbol

VEGFR