3-(1-Cyano-1-methylethyl)-N-[3-[(3,4-dihydro-3-methyl-4-oxo-6-quinazolinyl)amino]-4-methylphenyl]benzamide
3-(Cyano-dimethyl-methyl)-N-[4-methyl-3-(3-methyl-4-oxo-3,4-dihydro-quinazolin-6-ylamino)-phenyl]-benzamide
CAS: 878739-06-1
Molecular Formula: C27H25N5O2
3-(1-Cyano-1-methylethyl)-N-[3-[(3,4-dihydro-3-methyl-4-oxo-6-quinazolinyl)amino]-4-methylphenyl]benzamide - Names and Identifiers
3-(1-Cyano-1-methylethyl)-N-[3-[(3,4-dihydro-3-methyl-4-oxo-6-quinazolinyl)amino]-4-methylphenyl]benzamide - Physico-chemical Properties
| Molecular Formula | C27H25N5O2 |
| Molar Mass | 451.52 |
| Solubility | Soluble in DMSO, not in water |
| Appearance | powder |
| Color | white to beige |
| Storage Condition | -20°C |
| Use | AZ-628 is a selective, orally available Raf inhibitor with excellent pharmacokinetic properties and robust tumor growth inhibition in xenograft studies ( (IC50 values are 29, 34 and 105 nM for c-Raf1, B-RafV600E and wild-type B-Raf, respectively). AZ-628 inhibits growth, and induces cell cycle arrest and apoptosis in colon and melanoma cell lines with the B-RafV600E mutation. |
| Target | B-Raf；B-RafV600E；c-Raf-1 |
| In vitro study | AZ628 inhibits B- Raf, and effective inhibition of AZ628 at p-ERK1/2 levels was observed B- Raf treatment of M14 parental cell lines containing B- Raf with increasing concentrations of az628. Clones against AZ628 express increased CRAF. Increased CRAF expression is a potential mechanism for resistance to continuous AZ628 treatment, resulting in persistent activation of ERK1/2. Treatment with AZ628 in 1/3 of the az628-insensitive cell lines did not significantly inhibit p-ERK1/2 activity. AZ628 acts on M14 cells with resistance to AZ628 and does not inhibit the activation of ERK. AZ628 acts on malignant melanoma cells with NRAS mutation and effectively reduces the activation of ERK. |
3-(1-Cyano-1-methylethyl)-N-[3-[(3,4-dihydro-3-methyl-4-oxo-6-quinazolinyl)amino]-4-methylphenyl]benzamide - Risk and Safety
| Hazard Symbols | T - Toxic |
| Risk Codes | R25 - Toxic if swallowed R36/37/38 - Irritating to eyes, respiratory system and skin. |
| Safety Description | S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. S36/37/39 - Wear suitable protective clothing, gloves and eye/face protection. S45 - In case of accident or if you feel unwell, seek medical advice immediately (show the label whenever possible.) |
| UN IDs | UN 2811 6.1 / PGIII |
| WGK Germany | 3 |
3-(1-Cyano-1-methylethyl)-N-[3-[(3,4-dihydro-3-methyl-4-oxo-6-quinazolinyl)amino]-4-methylphenyl]benzamide - Reference
| Reference Show more | 1: Whittaker SR, Theurillat JP, Van Allen E, Wagle N, Hsiao J, Cowley GS, Schadendorf D, Root DE, Garraway LA. A genome-scale RNA interference screen implicates NF1 loss in resistance to RAF inhibition. Cancer Discov. 2013 Jan 3. [Epub ahead of print] PubMed PMID: 23288408. 2: Montagut C, Sharma SV, Shioda T, McDermott U, Ulman M, Ulkus LE, Dias-Santagata D, Stubbs H, Lee DY, Singh A, Drew L, Haber DA, Settleman J. Elevated CRAF as a potential mechanism of acquired resistance to BRAF inhibition in melanoma. Cancer Res. 2008 Jun 15;68(12):4853-61. doi: 10.1158/0008-5472.CAN-07-6787. PubMed PMID: 18559533; PubMed Central PMCID: PMC2692356. |
3-(1-Cyano-1-methylethyl)-N-[3-[(3,4-dihydro-3-methyl-4-oxo-6-quinazolinyl)amino]-4-methylphenyl]benzamide - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.215 ml | 11.074 ml | 22.147 ml |
| 5 mM | 0.443 ml | 2.215 ml | 4.429 ml |
| 10 mM | 0.221 ml | 1.107 ml | 2.215 ml |
| 5 mM | 0.044 ml | 0.221 ml | 0.443 ml |
Last Update：2024-01-02 23:10:35
3-(1-Cyano-1-methylethyl)-N-[3-[(3,4-dihydro-3-methyl-4-oxo-6-quinazolinyl)amino]-4-methylphenyl]benzamide - Reference Information
| biological activity | AZ 628 is a novel pan-Raf inhibitor that acts on BRAF, BRAF V600E and c-Raf-1, the IC50 was 105 nM, 34 nM and 29 nM, respectively, and also inhibited VEGFR2, DDR2, Lyn, Flt1, FMS, etc. AZ628 is a novel Pan-Raf inhibitor that acts on BRAF,BRAF V600E, and c-Raf-1 with IC50 of 105 nM,34 nM, and 29 nM, respectively, in cell-free assays and also inhibits VEGFR2, DDR2, Lyn, Flt1, FMS, etc. AZ628 can induce apoptosis. |
| 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 |
Last Update：2024-04-09 15:16:56
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Spot supply
Product Name: 3-(Cyano-dimethyl-methyl)-N-[4-methyl-3-(3-methyl-4-oxo-3,4-dihydro-quinazolin-6-ylamino)-phenyl]-benzamide Visit Supplier Webpage Request for quotationCAS: 878739-06-1
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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