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ChemicalBook > Product Catalogue >Biochemical Engineering >Inhibitors >protein tyrosine kinase >Apatinib

Apatinib

Apatinib Structure
  • ₹0
  • Product name: Apatinib
  • CAS: 811803-05-1
  • MF: C24H23N5O
  • MW: 397.47
  • EINECS:1592732-453-0
  • MDL Number:MFCD22420814
  • Synonyms:Apatinib;Apatinib (YN968D1);Aptinib;N-(4-(1-cyanocyclopentyl)phenyl)-2-(pyridin-4-ylMethylaMino)nicotinaMide;Mesylate APA;N-[4-(1-Cyanocyclopentyl)phenyl]-2-[(4-pyridinylmethyl)amino]-3-pyridinecarboxamide Apatinib;3-Pyridinecarboxamide, N-[4-(1-cyanocyclopentyl)phenyl]-2-[(4-pyridinylmethyl)amino]-;CS-1160
Properties Safety Information Description
Manufacturer Product number Product description Packaging Price Updated Buy

Properties

Boiling point :578.2±50.0 °C(Predicted)
Density :1.27
storage temp. :Store at -20°C
solubility :>49.4mg/ml in DMSO
form :Powder
pka :11.93±0.70(Predicted)

Safety Information

Symbol(GHS): GHS hazard pictograms
Signal word: Warning
Hazard statements:
Code Hazard statements Hazard class Category Signal word Pictogram P-Codes
H302 Harmful if swallowed Acute toxicity,oral Category 4 Warning GHS hazard pictograms P264, P270, P301+P312, P330, P501
H315 Causes skin irritation Skin corrosion/irritation Category 2 Warning GHS hazard pictograms P264, P280, P302+P352, P321,P332+P313, P362
H319 Causes serious eye irritation Serious eye damage/eye irritation Category 2A Warning GHS hazard pictograms P264, P280, P305+P351+P338,P337+P313P
H335 May cause respiratory irritation Specific target organ toxicity, single exposure;Respiratory tract irritation Category 3 Warning GHS hazard pictograms
Precautionary statements:
P261 Avoid breathing dust/fume/gas/mist/vapours/spray.
P264 Wash hands thoroughly after handling.
P264 Wash skin thouroughly after handling.
P270 Do not eat, drink or smoke when using this product.
P271 Use only outdoors or in a well-ventilated area.
P280 Wear protective gloves/protective clothing/eye protection/face protection.
P301+P312 IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.
P302+P352 IF ON SKIN: wash with plenty of soap and water.
P304+P340 IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.
P305+P351+P338 IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
P321 Specific treatment (see … on this label).
P330 Rinse mouth.
P332+P313 IF SKIN irritation occurs: Get medical advice/attention.
P337+P313 IF eye irritation persists: Get medical advice/attention.
P403+P233 Store in a well-ventilated place. Keep container tightly closed.
P405 Store locked up.
P501 Dispose of contents/container to..…

Description

Apatinib mesylate, discovered by Advenchen Laboratories (United States of America, USA) and co-developed by Jiangsu Hengrui Medicine Co. Ltd (China), was approved by the Chinese Food and Drug Administration (CFDA) in October 2014 for the treatment of metastatic gastric carcinoma. Apatinib mesylate is an oral tyrosine kinase inhibitor that selectively inhibits the vascular endothelial growth factor receptor 2 (VEGFR2), which prevents new blood vessel formation selectively in tumor tissue. Apatinib has shown inhibition of the VEGF signaling pathway with an IC50 value of 1 nM for VEGFR-2 in in vitro enzyme experiments. A multicenter phase II study of apatinib is underway with patients in non-triple-negative metastatic breast cancer trials. Non-clinical studies concluded that apatinib may reverse the ATP-binding cassette subfamily B member 1 and subfamily G member 2 (ABCB1- and ABCG2, respectively)-mediated multidrug resistance which allows cancer cells to circumvent certain conventional antineoplastic drugs, suggesting that apatinib could be effective as a combination therapy.

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