Benzamide, 3-(1-cyano-1-methylethyl)-N-[3-[(7-methoxy-4-quinazolinyl)amino]-4-methylphenyl]-
3-(2-cyanopropan-2-yl)-N-(3-((7-methoxyquinazolin-4-yl)amino)-4-methylphenyl)benzamide
CAS: 942507-42-8
Molecular Formula: C27H25N5O2
Benzamide, 3-(1-cyano-1-methylethyl)-N-[3-[(7-methoxy-4-quinazolinyl)amino]-4-methylphenyl]- - Names and Identifiers
Benzamide, 3-(1-cyano-1-methylethyl)-N-[3-[(7-methoxy-4-quinazolinyl)amino]-4-methylphenyl]- - Physico-chemical Properties
| Molecular Formula | C27H25N5O2 |
| Molar Mass | 451.52 |
| Density | 1.270±0.06 g/cm3(Predicted) |
| Boling Point | 582.6±50.0 °C(Predicted) |
| Solubility | DMSO: 85 mg/mLEthanol: 4 mg/mLWater: Insoluble( < 1 mg/ml refers to the product slightly soluble or insoluble) |
| pKa | 12.87±0.70(Predicted) |
| Storage Condition | -20°C |
| Use | AZ304 is a double inhibitor of BRAF, which effectively inhibits wild-type BRAF, mutant BRAF (V600E) and wild-type CRAF with IC50 values of 79 nM,38 nM and 68 nM respectively. AZ304 has a significant inhibitory effect on other kinases, such as p38 (IC50,6 nM),CSF1R (IC50,35 nM). |
| Target | B-RAF V600E; B-RAF; C-RAF; p38; CSF1R |
| In vitro study | AZ304 in vitro against wild-type BRAF and CRAF, BRAF. |
| In vivo study | In both RKO and Caco-2 tumor models, AZ304 alone or in combination with Cetuximab elicited antitumor activity without apparent toxic effects (regardless of BRAF mutation). |
Benzamide, 3-(1-cyano-1-methylethyl)-N-[3-[(7-methoxy-4-quinazolinyl)amino]-4-methylphenyl]- - Reference
| Reference Show more | 1. Ma R, et al. AZ304, a novel dual BRAF inhibitor, exerts anti-tumour effects in colorectal cancer independently of BRAF genetic status. Br J Cancer. 2018 May;118(11):1453-1463. |
Benzamide, 3-(1-cyano-1-methylethyl)-N-[3-[(7-methoxy-4-quinazolinyl)amino]-4-methylphenyl]- - 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
Benzamide, 3-(1-cyano-1-methylethyl)-N-[3-[(7-methoxy-4-quinazolinyl)amino]-4-methylphenyl]- - Cell Experiment
Briefly, the cells were treated with DMSO or multiple concentrations of AZ304 for 3 days. The cell growth was determined using the CellTiter 96 Aqueous One Cell Proliferation Assay. Percentage of net growth at day 3 (100%) relative to day 0 (0%) was calculated and the concentration of compound required to inhibit growth by 50% (GI50) determined. The assays were done in triplicate across different plates. The proliferation assays in selected colorectal cancer cell lines were measured using an MTT assay. First of all, cultured cells were seeded into 96-well plates (2000–5000 cells per well). After incubation for 24 h, the cells were pretreated with DMSO or AZ304 for 1 h. Then the indicated doses of Cetuximab were added. Cells were incubated for a further 48 or 72 h. For EGF stimulating assay, cells were incubated in reduced serum medium overnight and then treated with AZ304 or AZ304 + EGF (20 ng/ml) for 72 h. Twenty microliters of MTT solution (5 mg/ml) was added to each well followed by 4 h incubation at 37 °C
Last Update：2023-08-16 21:32:38
Benzamide, 3-(1-cyano-1-methylethyl)-N-[3-[(7-methoxy-4-quinazolinyl)amino]-4-methylphenyl]- - Animal Experiment
Female 4–6 weeks old athymic BALB/c nude mice were purchased from Shanghai SLAC Laboratory Animal Centre. RKO/Caco-2 cells (1 × 10^7) in 200 μl PBS were injected subcutaneously into the right scapular region of mice. After the average tumour size reached 150 – 200 mm^3, animals were randomly divided into 4 groups, each containing three mice and were treated with vehicle only (CON) which orally received 0.5% HPMC and injected with 0.9% saline, AZ304 only (AZ304 dissolved in 0.5% HPMC, 10 mg/kg by oral gavage twice daily), Cetuximab only (40 mg/kg by intraperitoneal injection twice per week), or their combination (A+C) for 10 days. Tumors were measured with a caliper every 2 days, so did body weights. Tumor volume was calculated using the formula V = 1/2 (width^2 × length). Mice were terminated by CO2 inhalation when the tumor diameters reached 1.5 cm, according to the protocol filed with the Guidance of Institutional Animal Care and Use Committee of China Medical University.
Last Update：2023-08-16 21:32:38
Benzamide, 3-(1-cyano-1-methylethyl)-N-[3-[(7-methoxy-4-quinazolinyl)amino]-4-methylphenyl]- - Introduction
3-(2-cyanopropan-2-yl)-N-(3-((7-methoxyquinazolin-4-yl)amino)-4-methylphenyl)benzamide is the name of a chemical substance, there are no details in my database for this compound. Generally speaking, to understand the properties, uses, preparation and safety information of a compound, we need to refer to the relevant chemical literature or database. You can provide more information about 3-(2-cyanopropan-2-yl)-N-(3-((7-methoxyquinazolin-4-yl)amino)-4-methylphenyl)benzamide so that I can find a more detailed answer for you.
Last Update：2024-04-10 22:29:15
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Product Name: 3-(2-cyanopropan-2-yl)-N-(3-((7-methoxyquinazolin-4-yl)amino)-4-methylphenyl)benzamide Visit Supplier Webpage Request for quotationCAS: 942507-42-8
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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