AZD9291DA HCl salt - CAS 1421372-66-8
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Not Intended for Therapeutic Use. For research use only.
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AZD9291-DA is a des acryl analogue of AZD9291, which is a third-generation EGFR inhibitor, showed promise in preclinical studies and provides hope for patients with advanced lung cancers that have become resistant to existing EGFR inhibitors. AZD9291 is highly active in preclinical models and is well tolerated in animal models.
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Brife Description:
third-generation EGFR inhibitor, the potential treatment of advanced lung cancers
brown solid powder
AZD9291-Des acryl analogue; AZD9291 Des acryl precursor; Mutated EGFR-IN-1; N1-(2-(dimethylamino)ethyl)-5-methoxy-N1-methyl-N4-(4-(1-methyl-1H-indol-3-yl)pyrimidin-2-yl)benzene-1,2,4-triamine; N1-(2-dimethylaminoethyl)-5-methoxy-N1-methyl-N4-[4-(1-methylindol-3-yl)pyrimidin-2-yl]benzene-1,2,4-triamine; SCHEMBL14660679
For research used only
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1.Hygroscopic growth of water-soluble matter extracted from remote marine aerosols over the western North Pacific: Influence of pollutants transported from East Asia.
Boreddy SK1, Kawamura K2. Sci Total Environ. 2016 Mar 23;557-558:285-295. doi: 10.1016/j.scitotenv.2016.03.096. [Epub ahead of print]
We examined the hygroscopic properties of water-soluble matter (WSM) nebulized from water extracts of total suspended particles (TSP) collected at Chichijima Island in the western North Pacific during January to September 2003. The hygroscopic growth factor g(RH) of the aerosol particles was measured using a hygroscopic tandem differential mobility analyzer (HTDMA) with an initial dry particle diameter of 100nm and relative humidity (RH) of 5-95%. The measured growth factor at 90% RH, g(90%), ranged from 1.51 to 2.14 (mean: 1.76±0.15), significantly lower than that of sea salts (2.1), probably owing to the heterogeneous reactions associated with chloride depletion in sea-salt particles and water-soluble organic matter (WSOM). The g(90%) maximized in summer and minimized in spring. The decrease in spring was most likely explained by the formation of less hygroscopic salts or particles via organometallic reactions during the long-range transport of Asian dust.
2.A hydrometallurgical process for recovering total metal values from waste monolithic ceramic capacitors.
Prabaharan G1, Barik SP2, Kumar B1. Waste Manag. 2016 Apr 12. pii: S0956-053X(16)30173-8. doi: 10.1016/j.wasman.2016.04.010. [Epub ahead of print]
A hydrometallurgical process for recovering the total metal values from waste monolithic ceramic capacitors was investigated. The process parameters such as time, temperature, acid concentration, hydrogen peroxide concentration and other reagents (amount of zinc dust and sodium formate) were optimized. Base metals such as Ba, Ti, Sn, Cu and Ni are leached out in two stages using HCl in stage 1 and HCl with H2O2 in stage 2. More than 99% of leaching efficiency for base metals (Cu, Ni, Ba, Ti and Sn) was achieved. Precious metals such as Au and Pd are leached out using aquaregia and nitric acid was used for the leaching of Ag. Base metals (Ba, Ti, Sn, Cu and Ni) are recovered by selective precipitation using H2SO4 and NaOH solution. In case of precious metals, Au and Pd from the leach solution were precipitated out using sodium metabisulphite and sodium formate, respectively. Sodium chloride was used for the precipitation of Ag from leach solution.
3.Characterizing the Dissolution Profiles of Supersaturable Salts, Cocrystals, and Solvates to Enhance In Vivo Oral Absorption.
Hisada N1, Takano R1, Takata N1, Shiraki K1, Ueto T1, Tanida S1, Kataoka M2, Yamashita S3. Eur J Pharm Biopharm. 2016 Apr 6. pii: S0939-6411(16)30128-X. doi: 10.1016/j.ejpb.2016.04.004. [Epub ahead of print]
The purposes of this study were to elucidate the type-specific characteristics of salt, cocrystal, and solvate formulations upon dissolution and precipitation, and to clarify their effect on enhancing oral absorption. Several types of solid formulations (dantrolene sodium salt [DAN-NA], pioglitazone hydrochloride salt [PIO-HCL], megestrol acetate saccharin cocrystal [MEG-SA], and an in-house compound ZR ethanolate [ZR-ETH]) that induce supersaturation of BCS class II drugs were compared to their crystalline free forms. An in vitro miniscale dissolution test in biorelevant media was used to characterize their dissolution profiles and residue forms. Both salts (DAN-NA and PIO-HCL) rapidly reached the maximum concentration within 5 minutes, whereas the cocrystal (MEG-SA) did so slowly. After the maximum concentration had been reached, the dissolved concentrations of DAN-NA, PIO-HCL, and MEG-SA decreased, but that of ZR-ETH did not. Time-dependent XRPD analysis revealed that the initial solid state of each salt dissolved within 5 minutes, whereas the cocrystal remained for more than 10 minutes, and the solvate remained for 4 hours.
4.Improving the yield of (+)-terrein from the salt-tolerant Aspergillus terreus PT06-2.
Zhao C1, Guo L1, Wang L2, Zhu G1, Zhu W3. World J Microbiol Biotechnol. 2016 May;32(5):77. doi: 10.1007/s11274-016-2029-0. Epub 2016 Apr 2.
(+)-Terrein has a potential application for drug discovery. To improve the yield of (+)-terrein, two-level Plackett-Burman design and response surface methodology methods were used to optimize the condition of a salt-tolerant fungus, Aspergillus terreus PT06-2. As a result, the yield of (+)-terrein reached 8.20 ± 0.072 g/L in a 500-mL flask containing 150 mL optimal medium consisted of 13.1 % NaCl, 3.6 % starch, 2 % sodium glutamate, 0.05 % KCl, 3 % inoculum size, adjusting initial pH value to 5 with 10 % HCl and shaking for 18 days at 28 °C and 180 rpm. The production of (+)-terrein was 47.0 % higher than the highest production reported in shake flasks. The advantages of this optimization are uses of single carbon source and nitrogen source and easy separation and purification by recrystallization. The result exhibited the potential and advantages of A. terreus PT06-2 in industrial production of (+)-terrein by fermentation.
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CAS 1421372-66-8 AZD9291DA HCl salt

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