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| Product Name: | AZ 628 | | Synonyms: | 3-(1-Cyano-1-methylethyl)-N-[3-[(3,4-dihydro-3-methyl-4-oxo-6-quinazolinyl)amino]-4-methylphenyl]benzamide;AZ-628;AZ628/AZ-628;AZD628;3-(2-cyanopropan-2-yl)-N-(4-methyl-3-(3-methyl-4-oxo-3,4-dihydroquinazolin-6-ylamino)phenyl)benzamide;AZ628, >=99%;3-(2-Cyanopropan-2-yl)-N-(4-methyl-3-((3-methyl-4-oxo-3,4-dihydroquinazolin-6-yl)amino)phenyl)ben;Benzamide, 3-(1-cyano-1-methylethyl)-N-[3-[(3,4-dihydro-3-methyl-4-oxo-6-quinazolinyl)amino]-4-methylphenyl]- | | CAS: | 878739-06-1 | | MF: | C27H25N5O2 | | MW: | 451.52 | | EINECS: | | | Product Categories: | Inhibitors;MAPK | | Mol File: | 878739-06-1.mol |  |
| | AZ 628 Chemical Properties |
| density | 1.21±0.1 g/cm3(Predicted) | | storage temp. | -20°C | | solubility | DMSO: soluble10mg/mL, clear | | form | powder | | pka | 12.92±0.70(Predicted) | | color | white to beige |
| Hazard Codes | T | | Risk Statements | 25-36/37/38 | | Safety Statements | 26-36/37/39-45 | | RIDADR | UN 2811 6.1 / PGIII | | WGK Germany | 3 | | HS Code | 2922500090 |
| | AZ 628 Usage And Synthesis |
| Uses | AZ 628 is an inhibitor of B-RAF and B-RAF(V600E) | | Definition | ChEBI: 3-(2-cyanopropan-2-yl)-N-[4-methyl-3-[(3-methyl-4-oxo-6-quinazolinyl)amino]phenyl]benzamide is a member of benzamides. | | Biological Activity | az628 is a potent and newly discorvered inhibitor of braf, c-raf-1 and brafv600e with ic50 values of 105 nm, 29 nm and 34 nm, respectively. this compound prevents craf activation through persistently occupying the atp-binding site of raf kinase. specificity profile suggests that az628 also inhibits activation of other tyrosine protein kinases such as ddr2, vegfr2, lyn, flt1, fms and others.raf kinases a family of three serine/threonine-specific protein kinases and participate in the ras-raf-mek-erk signal transduction cascade, also known as the mitogen-activated protein kinase (mapk) cascade. the activation of mapk signaling leads to different cellular response such as cell proliferation, apoptosis and inflammation.az628 has the potent anti-tumor activity. in human colon and melanoma-derived cell line that carries the recurrent v600e activating braf mutation, az628 was shown to inhibit anchorage-dependent and -independent growth, induce cell cycle arrest, and cause apoptosis [1]. az628 may be antiangiogenic due to inhibition of vegfr2 [2].generation of melanoma cell line clones is obtained resistance to the raf kinase inhibitor az628. resistance to az628 is connected with raised levels of the raf downstream effector p-erk1/2. erk1/2 initiation in az628-resistant clones is interceded by mek. supported multiplication of az628-resistant clones is to a great extent autonomous of braf kinase action. az628-resistant clones express elevated craf. survival of az628-safe cells is subject to craf [1]. | | in vitro | AZ628 inhibits B-Raf, B-Raf AZ628 acts on B-Raf-containing M14 parental cell lines treated with increasing concentrations of AZ628, an effective inhibition of p-ERK1/2 levels was observed. It acts on AZ628-resistant M14 cells and does not inhibit ERK activation. AZ628 acts on NRAS-mutated malignant melanoma cells and effectively reduces ERK activation. | | target | | Target | Value | C-Raf-1
(Cell-free assay) | 29 nM | B-Raf (V600E)
(Cell-free assay) | 34 nM | B-Raf
(Cell-free assay) | 105 nM |
| | storage | Store at +4°C | | references | 1. montagut c, sharma sv, shioda t, mcdermott u, ulman m, ulkus le, et al. elevated craf as a potential mechanism of acquired resistance to braf inhibition in melanoma. cancer res 2008,68:4853-4861.2. khazak v, astsaturov i, serebriiskii ig, golemis ea. selective raf inhibition in cancer therapy. expert opin ther targets 2007,11:1587-1609. |
| | AZ 628 Preparation Products And Raw materials |
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