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.

Chemical Structure

Apatinib mesylate
CAS# 1218779-75-9 (mesylate)

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

Size Price Shipping out time Quantity
100mg USD 150 Same Day
200mg USD 250 Same Day
500mg USD 450 Same Day
1g USD 850 Same Day
2g USD 1450 Same Day
5g USD 3250 Same Day
10g USD 5650 2 Weeks
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Pricing updated 2021-02-24. Prices are subject to change without notice.

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

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 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

white solid powder

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

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).

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).

HS Tariff Code:

Preparing Stock Solutions

The following data is based on the product molecular weight 493.58 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

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Additional Information

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).