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| | ZM 306416 Basic information |
| Product Name: | ZM 306416 | | Synonyms: | ZM 306416 HYDROCHLORIDE;4-[(4'-CHLORO-2'-FLUORO)PHENYLAMINO]-6,7-DIMETHOXYQUINAZOLINE HYDROCHLORIDE;4-QuinazolinaMine,N-(4-chloro-2-fluorophenyl)-6,7-diMethoxy-;ZM306416/ZM-306416;CB 676475;CB676475;CB-676475;ZM 213689 DisodiuM Salt (MeropeneM iMpurity) (Mixture of double bond isoMers) | | CAS: | 690206-97-4 | | MF: | C16H13ClFN3O2 | | MW: | 333.74 | | EINECS: | | | Product Categories: | Inhibitors;Angiogenesis and Metastasis | | Mol File: | 690206-97-4.mol |  |
| | ZM 306416 Chemical Properties |
| Melting point | >161°C (dec.) | | Boiling point | 434.1±45.0 °C(Predicted) | | density | 1.389±0.06 g/cm3(Predicted) | | storage temp. | Keep in dark place,Inert atmosphere,2-8°C | | solubility | Methanol (Slightly), Water (Sparingly) | | pka | 5.49±0.30(Predicted) | | form | Off-white solid. | | color | Light Orange to Brown | | Stability: | Hygroscopic |
| | ZM 306416 Usage And Synthesis |
| Uses | ZM-306416 is a VEGFR inhibitor, inhibiting Src, VEGFR1 and Abl with IC50 of 0.33 μM, 0.33 μM and 1.3 μM, respectively. | | Uses | ZM 306416 an inhibitor of tyrosine kinase RTK signaling pathway involved in anti-cancer agents. Anti-tumor, anti-metastatic agent. | | Uses | The major metabolite of Meropenem (M225620) - a carbapenem antibiotic - in plasma and urine. This metabolite existed as a mixture of 1-pyrroline and its 2-pyrroline isomer, and the coexistence of the two isomers at equilibrium in aqueous solutions was observed by NMR. | | Definition | ChEBI: N-(4-chloro-2-fluorophenyl)-6,7-dimethoxy-4-quinazolinamine is a member of quinazolines. | | Biological Activity | zm 306416 is a selective inhibitor of vegfr with ic50 value of 0.67μm [1]. it is also reported that zm 306416 inhibits egfr with ic50 value less than 10 nm [2].vascular endothelial growth factor receptor (vegfr) is a key element of the extracellular matrix(ecm) and plays an important role in angiogenesis cooperating with its ligand vegf. several studies have demonstrated that vegfrs expressed in liquid and solid tumor cells, such as nsclc, melanoma, prostate cancer, leukemia, mesothelioma, and breast cancer and are being regarded as a promising target in clinical [3].zm 306416 is a potent vegfr inhibitor and has a different selectivity with other reported vegfr inhibitors. using a549-egfrb cells for egfrb assay revealed that zm 306416 exhibited inhibitory activity on vegfr with ic50 value of 670 nm [1]. when tested with human thyroid follicular cells, zm 306416 treatment exhibited function on reducing vegfr2 phosphorylation and inhibiting endogenous, steady-state levels of p42/44 mapk phosphorylation [4]. | | target | VEGFR1 | | references | 1. antczak, c., et al., a high-content biosensor-based screen identifies cell-permeable activators and inhibitors of egfr function: implications in drug discovery. j biomol screen, 2012. 17(7): p. 885-99.2. choi kj, baik ih, ye sk et al. molecular targeted therapy for hepatocellular carcinoma: present status and future directions. biol pharm bull. 2015;38(7):986-91. 3. choi, k.j., et al., molecular targeted therapy for hepatocellular carcinoma: present status and future directions. biol pharm bull, 2015. 38(7): p. 986-91.4. susarla, r., j.c. watkinson, and m.c. eggo, regulation of human thyroid follicular cell function by inhibition of vascular endothelial growth factor receptor signalling. mol cell endocrinol, 2012. 351(2): p. 199-207. |
| | ZM 306416 Preparation Products And Raw materials |
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