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MedKoo product information:

 

Cabozantinib

   

Description of Cabozantinib: Cabozantinib, also known as XL-184 or BMS-907351, is an orally bioavailable, small molecule receptor tyrosine kinase (RTK) inhibitor with potential antineoplastic activity. Cabozantinib strongly binds to and inhibits several tyrosine receptor kinases. Specifically, cabozantinib appears to have a strong affinity for the hepatocyte growth factor receptor (Met) and vascular endothelial growth factor receptor 2 (VEGFR2), which may result in inhibition of tumor growth and angiogenesis, and tumor regression. Cabozantinib has also been shown to inhibit mast/stem cell growth factor (KIT), FMS-like tyrosine kinase 3 (Flt3) and tyrosine-protein kinase receptor (Tie-2). Cabozantinib was approved by the U.S. FDA in November 2012 for the treatment of medullary thyroid cancer. Check for active clinical trials/a> or closed clinical trials using this agent. (NCI Thesaurus).

   

MedKoo Cat#: 200595

Name: Cabozantinib

CAS#: 849217-68-1

Synonym: Cabozantinib, XL-184, XL184. BMS 907351; BMS-907351; BMS907351; trade name Cometriq

IUPAC/Chemical name: 

 N-{4-[(6,7-dimethoxyquinolin-4-yl)oxy]phenyl}-N'-(4-fluorophenyl)cyclopropane-1,1- dicarboxamide

Chemical structure

Theoretical analysis

MedKoo Cat#:  200595
Name:  Cabozantinib
CAS#:  849217-68-1

Chemical Formula: C28H24FN3O5

Exact Mass: 501.17000

Molecular Weight: 501.50

 Elemental Analysis: C, 67.06; H, 4.82; F, 3.79; N, 8.38; O, 15.95

 

Availability and price:

Cabozantinib (XL184, purity: 99%)  is in stock. Price updated on 08/14/2014). Delivery time: overnight (USA/Canada) or 3-5 day (international). Same day shipping from Chapel Hill, North Carolina, USA. Shipping fee: $30.00 (USA), $45.00 (Canada); $70.00 (international).

10mg / $150.00

25mg / $250.00

50mg / $350.00

100mg / $550.00

200mg / $650.00

500mg / $850.00

1.0g / $1,250.00

2.0g / $1,950.00

5.0g / ask price

Bulk available at low prices.

  

    

Technical data

Product data sheet

View product data sheet

Appearance:

white solid powder

Purity:

>98% (or refer to the Certificate of Analysis)

Certificate of Analysis:

View current batch of CoA

QC data:

View NMR, View HPLC, View MS

Safety Data Sheet (MSDS):

View Material Safety Data Sheet (MSDS)

Shipping condition:

Shipped under ambient temperature as non-hazardous chemical.  This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage condition:

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:

Soluble in DMSO, not in water

Shelf life:

>2 years if stored properly

Drug formulation:

This drug may be formulated in DMSO

Stock solution storage:

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Note: The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

    

Information about this agent

Cabozantinib (Marketed under the tradename Cometriq, formerly known as XL184) is a small molecule inhibitor of the tyrosine kinases c-Met and VEGFR2, and has been shown to reduce tumor growth, metastasis, and angiogenesis. It was developed by Exelixis Inc. Cabozantinib was granted orphan-drug status by the U.S. Food and Drug Administration (FDA) in January 2011. Cabozantinib was approved by the U.S. FDA in November 2012 for the treatment of medullary thyroid cancer[2] and it is currently undergoing clinical trials for the treatment of prostate, ovarian, brain, melanoma, breast, non-small cell lung, hepatocellular and kidney cancers. (source: http://en.wikipedia.org/wiki/Cabozantinib).

 

   

References

1: Hart CD, De Boer RH. Profile of cabozantinib and its potential in the treatment of advanced medullary thyroid cancer. Onco Targets Ther. 2013;6:1-7. doi: 10.2147/OTT.S27671. Epub 2013 Jan 3. PubMed PMID: 23319867; PubMed Central PMCID: PMC3540909.

2: Vaishampayan U. Cabozantinib as a Novel Therapy for Renal Cell Carcinoma. Curr Oncol Rep. 2013 Jan 5. [Epub ahead of print] PubMed PMID: 23292795.

3: Traynor K. Cabozantinib approved for advanced medullary thyroid cancer. Am J Health Syst Pharm. 2013 Jan 15;70(2):88. doi: 10.2146/news130005. PubMed PMID: 23292257.

4: Goodin S, Dipaola RS. Cabozantinib in prostate cancer: the beginning of a precision paradigm? J Clin Oncol. 2013 Feb 1;31(4):401-3. doi: 10.1200/JCO.2012.46.6185. Epub 2012 Dec 17. PubMed PMID: 23248244.

5: Smith DC, Smith MR, Sweeney C, Elfiky AA, Logothetis C, Corn PG, Vogelzang NJ, Small EJ, Harzstark AL, Gordon MS, Vaishampayan UN, Haas NB, Spira AI, Lara PN Jr, Lin CC, Srinivas S, Sella A, Schöffski P, Scheffold C, Weitzman AL, Hussain M. Cabozantinib in Patients With Advanced Prostate Cancer: Results of a Phase II Randomized Discontinuation Trial. J Clin Oncol. 2013 Feb 1;31(4):412-9. doi: 10.1200/JCO.2012.45.0494. Epub 2012 Nov 19. PubMed PMID: 23169517.

6: Nagilla M, Brown RL, Cohen EE. Cabozantinib for the treatment of advanced medullary thyroid cancer. Adv Ther. 2012 Nov;29(11):925-34. doi: 10.1007/s12325-012-0060-6. Epub 2012 Oct 25. PubMed PMID: 23104465.

7: Bowles DW, Kessler ER, Jimeno A. Multi-targeted tyrosine kinase inhibitors in clinical development: focus on XL-184 (cabozantinib). Drugs Today (Barc). 2011 Nov;47(11):857-68. doi: 10.1358/dot.2011.47.11.1688487. Review. PubMed PMID: 22146228.

8: Yakes FM, Chen J, Tan J, Yamaguchi K, Shi Y, Yu P, Qian F, Chu F, Bentzien F, Cancilla B, Orf J, You A, Laird AD, Engst S, Lee L, Lesch J, Chou YC, Joly AH. Cabozantinib (XL184), a novel MET and VEGFR2 inhibitor, simultaneously suppresses metastasis, angiogenesis, and tumor growth. Mol Cancer Ther. 2011 Dec;10(12):2298-308. doi: 10.1158/1535-7163.MCT-11-0264. Epub 2011 Sep 16. PubMed PMID: 21926191.

9: Kurzrock R, Sherman SI, Ball DW, Forastiere AA, Cohen RB, Mehra R, Pfister DG, Cohen EE, Janisch L, Nauling F, Hong DS, Ng CS, Ye L, Gagel RF, Frye J, Müller T, Ratain MJ, Salgia R. Activity of XL184 (Cabozantinib), an oral tyrosine kinase inhibitor, in patients with medullary thyroid cancer. J Clin Oncol. 2011 Jul 1;29(19):2660-6. doi: 10.1200/JCO.2010.32.4145. Epub 2011 May 23. PubMed PMID: 21606412.

10: Houvras Y, Wirth LJ. Cabozantinib in medullary thyroid carcinoma: time to focus the spotlight on this rare disease. J Clin Oncol. 2011 Jul 1;29(19):2616-8. doi: 10.1200/JCO.2010.34.0505. Epub 2011 May 23. PubMed PMID: 21606409.

11: Durante C, Russo D, Verrienti A, Filetti S. XL184 (cabozantinib) for medullary thyroid carcinoma. Expert Opin Investig Drugs. 2011 Mar;20(3):407-413. doi: 10.1517/13543784.2011.559163. Review. PubMed PMID: 21314233.

 

 

 

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