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- Wonjin Park, .et al. Human plasminogen-derived N-acetyl-Arg-Leu-Tyr-Glu antagonizes VEGFR-2 to prevent blood-retinal barrier breakdown in diabetic mice, Biomed Pharmacother, 2021, Feb;134:111110 PMID: 33338749
- Majid Momeny, .et al. Anti-tumour activity of tivozanib, a pan-inhibitor of VEGF receptors, in therapy-resistant ovarian carcinoma cells, Sci Rep, 2017, 7: 45954 PMID: 28383032
Biological Activity
Apatinib (YN968D1) is a tyrosine kinase inhibitor that selectively inhibits the vascular endothelial growth factor receptor-2 (VEGFR2, also known as KDR) that inhibits VEGF-mediated endothelial cell migration and proliferation thus blocking new blood vessel formation in tumor tissue.
Targets
| Target | Value |
|---|---|
| VEGFR2 | IC50: 1nM |
| RET | IC50: 13nM |
| c-Kit | IC50: 429nM |
| c-Src | IC50: 530nM |
| PDGFRα | IC50: >1μM |
| EGFR | IC50: >10μM |
| HER2 | IC50: >10μM |
| FGFR1 | IC50: >10μM |
| In vitro | DMSO | 77 mg/mL (193.72 mM) | |
| Water | Insoluble | ||
| Ethanol | 10 mg/mL | ||
|
* <1 mg/ml means slightly soluble or insoluble. * Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
|||
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.1 mM | 20.26 mL | 101.3 mL | 202.59 mL |
| 0.5 mM | 4.05 mL | 20.26 mL | 40.52 mL |
| 1 mM | 2.03 mL | 10.13 mL | 20.26 mL |
| 5 mM | 0.41 mL | 2.03 mL | 4.05 mL |
*The above data is based on the productmolecular weight 493.6 . Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Catalog Num | A11407 |
|---|---|
| Actions | Inhibitor |
| CAS No. | 811803-05-1 |
| Formula | C25H27N5O4S |
| M. Wt | 493.6 |
| Purity | >98% |
| 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 |
| Storage | Store lyophilized at -20ºC, keep desiccated. |
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