Cabozantinib malate
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MedKoo CAT#: 123216

CAS#: 1140909-48-3 (malate)

Description: Cabozantinib malate (XL-184 or BMS-907351) is the s-malate salt form of cabozantinib, an orally bioavailable, small molecule receptor tyrosine kinase (RTK) inhibitor with potential antineoplastic activity. Cabozantinib strongly binds to and inhibits several RTKs, which are often overexpressed in a variety of cancer cell types, including hepatocyte growth factor receptor (MET), RET (rearranged during transfection), vascular endothelial growth factor receptor types 1 (VEGFR-1), 2 (VEGFR-2), and 3 (VEGFR-3), mast/stem cell growth factor (KIT), FMS-like tyrosine kinase 3 (FLT-3), TIE-2 (TEK tyrosine kinase, endothelial), tropomyosin-related kinase B (TRKB) and AXL. This may result in an inhibition of both tumor growth and angiogenesis, and eventually lead to tumor regression. Cabozantinib was approved by the U.S. FDA in November 2012 for the treatment of medullary thyroid cancer.


Price and Availability

Size
Price

200mg
USD 90
2g
USD 450
20g
USD 1950
Size
Price

500mg
USD 150
5g
USD 850
50g
USD 3950
Size
Price

1g
USD 250
10g
USD 1450
100g
USD 5650

Cabozantinib malate purity > 98%, is in stock. The same day shipping out after order is received. Note: the estimated shipping out time for order > 50g may be 2 weeks.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 123216
Name: Cabozantinib malate
CAS#: 1140909-48-3 (malate)
Chemical Formula: C32H30FN3O10
Exact Mass:
Molecular Weight: 635.6014
Elemental Analysis: C, 60.47; H, 4.76; F, 2.99; N, 6.61; O, 25.17


Related CAS #: 1140909-48-3 (malate)   849217-68-1 (free base)    

Synonym: XL-184; XL184; XL 184; BMS907351; BMS 907351; BMS-907351; Cabozantinib malate; Cabozantinib S-malate. Brand name: Cometriq.

IUPAC/Chemical Name: N-(4-((6,7-dimethoxyquinolin-4-yl)oxy)phenyl)-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide (S)-2-hydroxysuccinate

InChi Key: HFCFMRYTXDINDK-WNQIDUERSA-N

InChi Code: InChI=1S/C28H24FN3O5.C4H6O5/c1-35-24-15-21-22(16-25(24)36-2)30-14-11-23(21)37-20-9-7-19(8-10-20)32-27(34)28(12-13-28)26(33)31-18-5-3-17(29)4-6-18;5-2(4(8)9)1-3(6)7/h3-11,14-16H,12-13H2,1-2H3,(H,31,33)(H,32,34);2,5H,1H2,(H,6,7)(H,8,9)/t;2-/m.0/s1

SMILES Code: COC1=CC2=C(OC3=CC=C(NC(C4(C(NC5=CC=C(F)C=C5)=O)CC4)=O)C=C3)C=CN=C2C=C1OC.O=C(O)[C@@H](O)CC(O)=O


Technical Data

Appearance:
Solid powder

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

Certificate of Analysis:

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

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).

Harmonized System Code:
293490


Additional Information

Related:
1140909-48-3 (Cabozantinib malate salt)
849217-68-1 (Cabozantinib free base).


References

1: Weitzman SP, Cabanillas ME. The treatment landscape in thyroid cancer: a focus on cabozantinib. Cancer Manag Res. 2015 Aug 19;7:265-78. doi: 10.2147/CMAR.S68373. eCollection 2015. Review. PubMed PMID: 26316818; PubMed Central PMCID: PMC4547654.

2: Zhang B, Zhang X, Zhou T, Liu J. Clinical observation of liver cancer patients treated with axitinib and cabozantinib after failed sorafenib treatment: a case report and literature review. Cancer Biol Ther. 2015;16(2):215-8. doi: 10.4161/15384047.2014.962318. Review. PubMed PMID: 25668362; PubMed Central PMCID: PMC4622678.

3: Fay AP, Albiges L, Bellmunt J. Current role of cabozantinib in metastatic castration-resistant prostate cancer. Expert Rev Anticancer Ther. 2015 Feb;15(2):151-6. doi: 10.1586/14737140.2015.1003047. Epub 2015 Jan 14. Review. PubMed PMID: 25586337.

4: Roy S, Narang BK, Rastogi SK, Rawal RK. A novel multiple tyrosine-kinase targeted agent to explore the future perspectives of anti-angiogenic therapy for the treatment of multiple solid tumors: cabozantinib. Anticancer Agents Med Chem. 2015;15(1):37-47. Review. PubMed PMID: 25181996.

5: Hoy SM. Cabozantinib: a review of its use in patients with medullary thyroid cancer. Drugs. 2014 Aug;74(12):1435-44. doi: 10.1007/s40265-014-0265-x. Review. PubMed PMID: 25056653.

6: Nix NM, Braun K. Cabozantinib for the treatment of metastatic medullary thyroid carcinoma. J Adv Pract Oncol. 2014 Jan;5(1):47-50. Review. PubMed PMID: 25032033; PubMed Central PMCID: PMC4093460.

7: Colombo JR, Wein RO. Cabozantinib for progressive metastatic medullary thyroid cancer: a review. Ther Clin Risk Manag. 2014 May 28;10:395-404. doi: 10.2147/TCRM.S46041. eCollection 2014. Review. PubMed PMID: 24920914; PubMed Central PMCID: PMC4043815.

8: Vaishampayan UN. Development of cabozantinib for the treatment of prostate cancer. Core Evid. 2014 Apr 23;9:61-7. doi: 10.2147/CE.S48498. eCollection 2014. Review. Erratum in: Core Evid. 2014;9:69. PubMed PMID: 24790591; PubMed Central PMCID: PMC4003147.

9: Grüllich C. Cabozantinib: a MET, RET, and VEGFR2 tyrosine kinase inhibitor. Recent Results Cancer Res. 2014;201:207-14. doi: 10.1007/978-3-642-54490-3_12. Review. PubMed PMID: 24756794.

10: Pinto A. Cabozantinib: a novel agent with a dual mechanism of action for castration-resistant prostate carcinoma. Cancer Chemother Pharmacol. 2014 Feb;73(2):219-22. doi: 10.1007/s00280-013-2343-2. Epub 2013 Nov 8. Review. PubMed PMID: 24202668.

11: Karras S, Pontikides N, Krassas GE. Pharmacokinetic evaluation of cabozantinib for the treatment of thyroid cancer. Expert Opin Drug Metab Toxicol. 2013 Apr;9(4):507-15. doi: 10.1517/17425255.2013.780028. Review. PubMed PMID: 23488614.

12: 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. Review. PubMed PMID: 23104465.

13: 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.

14: 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.