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Osimertinib (AZD-9291) phofo

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SKU: 1421373-65-0. Category:

AASraw e na le bokhoni ba tlhahiso le tlhahiso ho tloha ho gram ho ea ka taelo e kholo ea phofo ea Osimertinib (AZD-9291) (1421373-65-0), tlas'a taolo ea CGMP le tsamaiso ea tšebetso ea boleng bo tsitsitseng.

Phororo ea Osimertinib (AZD-9291) ke molomo, etsolloa sesitisa tsa epidermal kgolo ya ntlha e receptor (EGFR) sensitizing le T790M hanyetsa liphetoho liphatseng tsa lefutso (IC50s = 15-17 NM) ha o qenehela tse hlaha-mofuta foromo ya receptor le (IC50 = 480 NM) .1 Ho tlama IGF1R amanang le hERG receptors le fokotswa implantency (IC50s = 2.9 le 16.2 μm, ka ho latellana) .1 AZD 9291 e se e bontšitse hore ho thibela metsoako kgolo ya hlahala ka mohlala xenograft toeba ka tekanyetso molomo oa 5-10 MG / lik'hilograma le lekiloeng ea bongaka ka ho bakuli ba ka e leng kankere e phahameng ea EGFR e seng e nyenyane-cell kankere.

Tlhaloso ea Sehlahisoa

Video ea phofo ea Osimertinib (AZD-9291)


Phororo ea Osimertinib (AZD-9291) tsebo ea motheo

Name: Phororo ea Osimertinib (AZD-9291)
CAS: 1421373-65-0
Molecular Formula: C28H33N7O2
Boima ba 'mele: 499.61
Melt Point: > 188ºC
Temp Temp Storage: -20 ° C
Color: Pente e le 'mala o mosehla o moputsoa


Osimertinib (AZD-9291) phofo e sebelisitsoeng

lebitso

AZD-9291 powder (CAS 1421373-65-0), N-[2-[[2-(dimethylamino)ethyl]methylamino]-4-methoxy-5-[[4-(1-methyl-1H-indol-3-yl)-2-pyrimidinyl]amino]phenyl]-2-propenamide

Sebeliso ea poula ea AZD-9291

AZD-9291 phofo laolwa hang letsatsi le letsatsi ka molomo ka 5 mg, / lik'hilograma bakileng bofokoli bo tebileng ba lihlahala ka mose EGFRm + (PC9; 178% kgolo ya thibelo) le EGFRm + / T790M (H1975; 119% kgolo ya thibelo) dikai hlahala ka vivo,
ka mor'a matsatsi a 14 dosing. Ho feta moo 5 mg / kg AZD-9291 phofo e ne e lekane ho baka ho fokotsa ho matla ha EGFRm + le EGFRm + / T790M transgenic mouse lung lung. Bothata ba ho thibela mokokotlo bo ne bo amahanngoa le ho thibela ho hoholo ha phosphorylation ea EGFR le litsela tse kholo tse tlaase tse kang AKT le ERK. Foleng ka nako e telele kalafo ya PC9 le H1975 xenograft lihlahala le AZD-9291 phofo ile sa etsa hore e feletseng le matlafatsa ka karabelo macroscopic, ho se lihlahala bonahalang ka mor'a matsatsi a 40 dosing, 'me le ntse a lula ka nģ'ane ho matsatsi a 100. Ho feta moo, dintlha tsa pele ho kliniki li boetse li bonts'a hore phofo ea AZD-9291 e ka lebisa lihlahala tse fumanoeng ho hanyetsa mokhoa oa HER2-amplification o sa tsoa tsebahatsoa, ​​e leng se ka fetisang melemo ea sona ho bakuli ba nang le lithibela-hloko tsa TKI.

Temoso ho phofo ea AZD-9291

AZD-9291 phofo (CAS 1421373-65-0) ke eona feela meriana e amohelehang e bontšitsoeng bakeng sa bakuli ba nang le metsoako ea EGFR T790M e nang le phetoho ea kokoana-hloko e seng e nyane ea kankere ea matšoafo. Pontšo ena e amoheloa tlas'a ts'ebetso ea FDA ea tumello e potlakileng ka lebaka la tekanyo ea likarabo tsa likarolo le nako ea karabo (DoR).

Litholoana tse tloaelehileng tse tloaelehileng li kenyeletsa letšollo, stomatitis, rashes, letlalo le omeletseng kapa le letle, mafu ao ho nang le monoana kapa litšepe ho khelosa letlalo, lipalo tse tlaase tsa platelete, litekanyo tse tlaase tsa lekocyte le litekanyo tse tlaase tsa neutrophile.
Ha ho na lipelaelo tsa TAGRISSO
Maloetse a Lung a Mangata (ILD) / Pneumonitis e etsahetse 3.3% mme a bolaea 0.5% ea bakuli ba 813 TAGRISSO. Qoba TAGRISSO 'me u batlisise hang-hang bakeng sa ILD ho mokuli leha e le ofe ea hlahisang ka ho mpefala ha matšoao a phefumolohang a bontšang ILD (mohlala, dyspnea, khohlela le feberu). Qoba ka ho sa feleng TAGRISSO haeba ILD e tiisoa
Qetello ea nako ea QTc e etsahetse bakuli ba TAGRISSO. Har'a bakuli ba 411 liphuputsong tse peli tsa Phase II, mokuli a le mong (0.2%) o fumanoe a e-na le QTc e kholo ho feta 500 msec, mme bakuli ba 11 (2.7%) ba na le keketseho ho tloha qalong ea QTc e kholo ho feta 60 msec. Ho itlhokomela ka nako le nako le li-ECG le electrolyte ho bakuli ba nang le lefu la qtc la congenital, congestive heart failure, ho se sebetse ha electrolyte, kapa ba noang meriana e tsejoang ho lelefatsa nako ea QTc. Ho khaotsa ka ho sa feleng TAGRISSO ho bakuli ba hlahisang nako ea nako ea QTc le lipontšo / matšoao a bophelo bo sokelang
Ho kula ha pelo ho ile ha etsahala ka 1.4% 'me ba bolaea 0.2% ea bakuli ba 813 TAGRISSO. Sepheo sa Left Ventricular Ejection (LVEF) se fokotseha> 10% le lerotholi ho <50% se etsahetse 2.4% ea (9 / 375) TAGRISSO bakuli. Hlahloba LVEF pele ho qaloa 'me ka nako ea likhoeli tsa 3 kalafo. Qoba TAGRISSO haeba karoloana ea ejection e fokotseha ka 10% ho tloha mekhoeng ea ho itšireletsa pele 'me e ka tlaase ho 50%. Bakeng sa matšoao a lefu la pelo a fokolang kapa a sa tsitsitseng a sa sebetsane le LV ka libeke tse 4, tlohela ka ho feletseng TAGRISSO.
Ho eletsa bakhachane monyetla oa ho ba lesea. Ho eletsa basali ba nang le bokhoni ba ho ikatisa ho sebelisa thibelo ea bokhachane e sebetsang nakong ea TAGRISSO kalafo le libeke tse 6 ka mor'a tekanyo ea ho qetela. Ho eletsa banna le basali ba nang le bokhoni ba ho ikatisa ho sebelisa likhokahano tse atlehang likhoeling tsa 4 ka mor'a tekanyo ea ho qetela.
Liphetoho tse tloaelehileng ka ho fetisisa (> 20%) tse hlokomelitsoeng ka TAGRISSO bakuli ba ne ba letshollo (42%), lihlahisoa (41%), letlalo le omeletseng (31%) le toxicity ea nail (25%).

Litaelo tse ling

AZD-9291 phofo e ne e le mafolofolo haholo ho bakuli ba nang le kankere ea matšoafo le phetoho ea EGFR T790M e neng e kile ea e-ba le tsoelo-pele ea mafu nakong ea pele ho phekoloa ka EGFR tyrosine kinase inhibitors.

Peso ea AZD-9291 e ntse e ithutoa nyeoeng e tiileng, AURA3, lengolo le bulehileng, tlhahlobo e hlakileng ea Phase III e reretsoeng ho hlahloba katleho le polokeho ea phofo ea AZD-9291 le dipatinate e thehiloeng ho doublet chemotherapy ho bakuli ba nang le EGFR T790M e ntle, kapa metastatic NSCLC ba tsoetseng pele kalafo e latelang pele le EGFR-TKI. AZD-9291 phofo e boetse e ntse e phenyekolloa ka mokhoa o amohelehang le sethaleng sa meeli ea pele, ho akarelletsa le bakuli ba nang le metastase ea boko, hammoho le ho kopana le metsoako e meng.

AZD-9291 phofo 80mg ha letsatsi le leng le le leng ke letlapa la pele le bontšitsoeng bakeng sa phekolo ea bakuli ba nang le metastatic epidermal growth factor receptor (EGFR) kankere ea matšoao e feto-fetoheng ea kankere ea matšoafo (NSCLC), e fumanoeng ke FDA-e amohelehang. teko, ba ileng ba hatela pele kapa ka mor'a lefuba la EGFR la tyrosine kinase inhibitor (TKI). Liphuputso tsa ma-vitro tse sa etsoang ke lingaka li bontšitse hore phofo ea AZD-790 e na le matla a phahameng a ho thibela phekolo ea EGFR ea phosphorylation ho pholletsa le mefuta ea EGFRm e sebetsang le ea methapo ea lisele ea NSCLC e nang le phetoho e nang le likarolo tse seng kae tse nyenyane khahlanong le EGFR melaong ea sele.

Osimertinib powder e sa tsoa hatisoa ke Mokhatlo oa Lefatše oa Bophelo (WHO) e le Lebitso la Machaba le se Nang Moahi (INN) la phofo ea AZD-9291, 'me e ka amoheloa ka molao nakong ea November 2015. US, Mokhatlo oa Amerika oa Meriana o ile oa amohela phofo ea Osimertinib e le lebitso la United States le amoheletsoeng (USAN).

Powder ea AZD-9291 (CAS 1421373-65-0)

Ntho e nyenyane 10grams.
Tlhahlobo ka bongata bo tloaelehileng (ka hare ho 1kg) e ka romeloa lihora tse 12 kamora ho lefa.
Bakeng sa tlhahiso e kholo (ka hare ho 1kg) e ka romeloa ka matsatsi a sebetsang a 3 ka mor'a ts'ebetso.

Caffeic Acid Phenethyl Ester Marketing

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Joang ho reka phofo ea Osimertinib; reka powder AZD-9291 (CAS 1421373-65-0) ho tloha AASraw

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COA

COA 1421373-65-0 Osimertinib (AZD-9291) AASRAW

HNMR

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