Apatinib mesylate
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MedKoo CAT#: 200135

CAS#: 1218779-75-9 (mesylate)

Description: Apatinib, also known as Rivoceranib, is an orally bioavailable, small-molecule receptor tyrosine kinase inhibitor with potential antiangiogenic and antineoplastic activities. The free-base form is also known as Rivoceranib. Apatinib selectively binds to and inhibits vascular endothelial growth factor receptor 2, which may inhibit VEGF-stimulated endothelial cell migration and proliferation and decrease tumor microvessel density. In addition, this agent mildly inhibits c-Kit and c-SRC tyrosine kinases.


Price and Availability

Size
Price

100mg
USD 150
1g
USD 850
10g
USD 5650
Size
Price

200mg
USD 250
2g
USD 1450
Size
Price

500mg
USD 450
5g
USD 3250

Apatinib mesylate, purity > 98%, is in stock. The same day shipping out after order is received.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 200135
Name: Apatinib mesylate
CAS#: 1218779-75-9 (mesylate)
Chemical Formula: C25H27N5O4S
Exact Mass:
Molecular Weight: 493.58
Elemental Analysis: C, 60.83; H, 5.51; N, 14.19; O, 12.97; S, 6.50


Related CAS #: 1218779-75-9 (mesylate)   811803-05-1 (free base)    

Synonym: YN-968D1; YN 968D1; YN968D1; Rivoceranib; Apatinib; Apatinib mesylate.

IUPAC/Chemical Name: N-(4-(1-cyanocyclopentyl)phenyl)-2-((4-methylpyridin-3-yl)amino)nicotinamide methanesulfonate

InChi Key: BDGPIQYIFFSTGI-UHFFFAOYSA-N

InChi Code: InChI=1S/C24H23N5O.CH4O3S/c1-17-10-14-26-15-21(17)29-22-20(5-4-13-27-22)23(30)28-19-8-6-18(7-9-19)24(16-25)11-2-3-12-24;1-5(2,3)4/h4-10,13-15H,2-3,11-12H2,1H3,(H,27,29)(H,28,30);1H3,(H,2,3,4)

SMILES Code: O=C(NC1=CC=C(C2(C#N)CCCC2)C=C1)C3=C(NC4=C(C)C=CN=C4)N=CC=C3.CS(=O)(O)=O


Technical Data

Appearance:
white 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, 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).

Harmonized System Code:
2934990300


Additional Information

Related:
1218779-75-9 (Apatinib mesylate salt)
811803-05-1 (Apatinib free base).

Apatinib, also known as YN968D1, is a tyrosine kinase inhibitor that selectively inhibits the vascular endothelial growth factor receptor-2 (VEGFR2, also known as KDR). It is an orally bioavailable, small molecule agent which is thought to inhibit angiogenesis in cancer cells; specifically apatinib inhibits VEGF-mediated endothelial cell migration and proliferation thus blocking new blood vessel formation in tumor tissue. This agent also mildly inhibits c-Kit and c-SRC tyrosine kinases. 
 
History of Apatinib: Apatinib was first synthesized by Advenchen Laboratories in California, USA and is being developed by Jiangsu Hengrui Medicine (China), LSK BioPartners (US) and Bukwang Pharmaceutical Company (Korea). It is an investigational cancer drug currently undergoing clinical trials as a potential targeted treatment for metastatic gastric carcinoma, metastatic breast cancer and advanced hepatocellular carcinoma. (source: http://en.wikipedia.org/wiki/Apatinib).
 
Development status of Apatinib: There is a Phase II/III study recruiting patients in China to determine whether apatinib can improve progression free survival compared with placebo in patients with metastatic gastric carcinoma who have failed two lines of chemotherapy (September, 2009). As of November, 2010, two additional Phase 2 clinical studies have been initiated for apatinib in metastatic triple-negative breast cancer patients and advanced hepatocellular carcinoma. On March 7, 2011, Bukwang announced that it filed an IND to the Korean FDA to begin Human clinical studies of Apatinib in Phase 2.  (source: http://en.wikipedia.org/wiki/Apatinib). 
  


References

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