Apatinib
Apatinib （YN968D1）is a potent inhibior of the VEGF signaling pathway with the IC50 value of 1nM for VEGFR-2 in in vitro enzyme experiments [1].
In vitro, Apatinib has shown the inhibition of tyrosine kinase activities with the IC50 values of 0.013μM, 0.429μM and 0.53μM for Ret, c-kit and c-src, respectively. In addition, Apatinib has been revealed to have no significant effects in EGFR, Her-2 or FGFR1 in concentrations up to 10μM. Apart from these, Apatinib has been reported to inhibit the growth factor-stimulated receptor phosphorylation at the cellular level. Furthermore, Apatinib has also reported to slightly inhibitor proliferation of HUVEC by 20% FBS with the IC50 value of 23.4μM and significantly inhibit stimulated by 20ng/mL VEGF with the IC50 value of 0.17μM. Once-daily oral administration of Apatinib has been noted to produce a dose-dependent inhibition of tumor growth in human tumor xenografts in immunodeficient mice [1]
References:
[1] Tian S1, Quan H, Xie C, Guo H, Lü F, Xu Y, Li J, Lou L. YN968D1 is a novel and selective inhibitor of vascular endothelial growth factor receptor-2 tyrosine kinase with potent activity in vitro and in vivo. Cancer Sci. 2011 Jul;102(7):1374-80.
.
- 1. ZiliangWang, Wei Chen, et al. "The Fibrillin‐1/VEGFR2/STAT2 signaling axis promotes chemoresistance via modulating glycolysis and angiogenesis in ovarian cancer organoids and cells." Cancer Commun (Lond). 2022 Mar;42(3):245-265. PMID:35234370
- 2. Zhong W, Jin W, et al. "Pioglitazone Induces Cardiomyocyte Apoptosis and Inhibits Cardiomyocyte Hypertrophy Via VEGFR-2 Signaling Pathway." Arq Bras Cardiol. 2018 Jul 2. pii: S0066-782X2018005008102. PMID:29972411
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 493.58 |
| Cas No. | 1218779-75-9 |
| Formula | C25H27N5O4S |
| Solubility | ≥49.4 mg/mL in DMSO; insoluble in H2O; ≥2.17 mg/mL in EtOH with gentle warming and ultrasonic |
| Chemical Name | N-[4-(1-cyanocyclopentyl)phenyl]-2-(pyridin-4-ylmethylamino)pyridine-3-carboxamide;methanesulfonic acid |
| SDF | Download SDF |
| Canonical SMILES | CS(=O)(=O)O.C1CCC(C1)(C#N)C2=CC=C(C=C2)NC(=O)C3=C(N=CC=C3)NCC4=CC=NC=C4 |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment [1]: | |
|
Cell lines |
HUVEC (human umbilical vein endothelial cells) |
|
Preparation method |
Limited solubility. General tips for obtaining a higher concentration: Please warm the tube at 37°C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months. |
|
Reaction Conditions |
37°C |
|
Applications |
In HUVEC, Apatinib decreases VEGF-stimulated phosphorylation of VEGFR-2 KDR in a concentration-dependent manner. It also completely inhibits VEGFR-2 activation at a concentration of 0.1 μM. Furthermore, Apatinib abrogates the phosphorylation of c-kit and PDGFRb in Mo7e and NIH-3T3 cells stimulated with the relevant ligand, respectively, in a concentration-dependent manner. In addition, Apatinib inhibits proliferation, migration and tube formation of HUVEC in vitro and blocking of rat aortic ring budding. |
| Animal experiment [1]: | |
|
Animal models |
Nude mice human tumor xenografts |
|
Dosage form |
Once daily by oral gavage |
|
Preparation method |
Diluted in 0.5% (w / v) carboxymethyl cellulose and 5% (w / v) glucose solution. |
|
Applications |
Apatinib inhibits growth of established NCI-H460 human lung tumors, HCT 116 human colon tumors, or SGC-7901 human gastric tumors in nude mice. Apatinib in combination with docetaxel or oxaliplatin exerts synergistic tumor growth inhibition effects against NCI-H460 and Ls174t xenografts, respectively. Apatinib also significantly suppresses angiogenesis in NCI-H460 xenograft tumor tissues. |
|
Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
|
References: 1. Tian S, Quan H, Xie C et al. YN968D1 is a novel and selective inhibitor of vascular endothelial growth factor receptor-2 tyrosine kinase with potent activity in vitro and in vivo. Cancer Sci. 2011 Jul;102(7):1374-80. |
|
| Description | Apatinib is an orally bioavailable, selective inhibitor of VEGFR2 with an IC50 value of 1 nM. | |||||
| Targets | VEGFR2 | RET | c-Kit | c-Src | PDGFRα | |
| IC50 | 1 nM | 13 nM | 429 nM | 530 nM | >1 μM | |
Quality Control & MSDS
- View current batch:
Chemical structure
Related Biological Data
Related Biological Data
Related Biological Data
