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XL-184

Cat. No. M1757
XL-184 Structure
Synonym:

Cabozantinib, BMS-907351

Size Price Availability Quantity
5mg USD 87 In stock
10mg USD 120 In stock
50mg USD 300 In stock
100mg USD 440 In stock
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Quality Control
Biological Activity

XL184 is a small molecule designed to inhibit multiple receptor tyrosine kinases, specifically MET and VEGFR2. MET is a receptor tyrosine kinase that plays key roles in cellular proliferation, migration, and invasion as well as angiogenesis. These biological processes contribute to the transformation, progression, survival and metastasis of cancer cells. The MET pathway is frequently activated in tumors through MET amplification, mutation, and overexpression, as well as through overexpression of its ligand HGF. Expression of VEGF has been observed in a variety of cancers and has been associated with the stimulation and growth of new blood vessels to support the tumor. MET and VEGFR2 are important driving forces in angiogenesis, implicated in the ability of tumors to overcome hypoxia following angiogenesis inhibition.

Protocol
Cell Experiment
Cell lines ST-88, STS26T and MPNST724 cells line
Preparation method Cell growth assays
MTS assays: these were conducted using CellTiter96 Aqueous Non-Radioactive Cell Proliferation Assay kit (Promega Corp, Madison, WI), per manufacturer's instructions. Drugs were administered at doses and for intervals as indicated. Absorbance was measured at a wavelength of 490 nm, and the absorbance values of treated cells are presented as a percentage of the absorbance of untreated cells. Colony formation assay: one hundred viable cells per well were plated and allowed to grow in normal medium for 10 days and then stained for 30 min at room temperature with a 6% glutaraldehyde, 0.5% crystal violet solution. Pictures were captured digitally and colonies were counted. All experiments were repeated at a minimum twice for each cell line.
Concentrations 0~10 µ M
Incubation time 48 h
Animal Experiment
Animal models SCID mice bearing STS26T and MPNST724 xenografts
Formulation not mentioned
Dosages 30mg/kg/d
Administration gavage
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 501.51
Formula C28H24FN3O5
CAS Number 849217-68-1
Purity >99%
Solubility DMSO
Storage at -20°C
References

Multi-targeted tyrosine kinase inhibitors in clinical development: focus on XL-184 (cabozantinib).
Bowles DW et al. Drugs Today (Barc). 2011 Nov;47(11):857-68. PMID: 22146228.

Cabozantinib (XL184), a novel MET and VEGFR2 inhibitor, simultaneously suppresses metastasis, angiogenesis, and tumor growth.
Yakes FM et al. Mol Cancer Ther. 2011 Dec;10(12):2298-308. PMID: 21926191.

Activity of XL184 (Cabozantinib), an oral tyrosine kinase inhibitor, in patients with medullary thyroid cancer.
Kurzrock R et al. J Clin Oncol. 2011 Jul 1;29(19):2660-6. PMID: 21606412.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: XL-184, Cabozantinib, BMS-907351 supplier, c-Met, inhibitors

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