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Buparlisib (944396-07-0)

Akukho kalo
5.00 ngaphandle kwe 5 ngenxa ye 1 ireyithingi abathengi
SKU: 944396-07-0. Udidi:

I-AASraw ikunye kunye nokukwazi ukuvelisa kwigram ukuya ku-Buparlisib (i-CAS 944396-07-0), phantsi komgaqo weCGMP kunye nolawulo lwekhwalithi ephezulu.

Buparlisib powder ngumlomo, ongenakufumaneka, ngokucacileyo, kunye ne-inhibitor enamandla ye-pan-class I phosphatidylinositol 3-kinase (PI3K) intsapho, kwaye inxaxheba yayo njengommeli we-antiticancer okwangoku uphando.

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Buparlisib Abalinganiswa basisiseko

igama: Buparlisib
CAS: 944396-07-0
I-molecular Formula: C18H21F3N6O2
Isisindo somzimba: 410.3935496
Melt Point: 645.7 ± 65.0 ° C
Isitoreji sokugcina: -20 ° C
umbala: Powstalline powder


Ukusetyenziswa kweBuparlisib (944396-07-0) kumjikelezo we-steroids

Amagama

I-Buparlisib (944396-07-0), i-pan-class I-phosphotidyinositol-3-kinase (PI3K) inhibitor.

Cancer Clinic

① Ingingqi

I-Buparlisib iyi-pan-class oral I-phosphotidyinositol-3-kinase (PI3K) inhibitor. Isigaba samanje ndihlola ukuvavanya ukhuseleko, i-pharmacokinetics, kunye nokusebenza kwe-buparlisib kunye ne-capecitabine kwizigulane ezine-metastatic cancer.

② Izigulane kunye neendlela
Izigulane zifumene i-buparlisib kanye imihla ngemihla (uluhlu, i-50 ukuya kwi-100 mg) kwiiveki ze-3 nge-capecitabine kabini imihla ngemihla (u-1000 ukuya ku-1250 mg / m2) kwiiveki ze-2 ezinekhefu ze-1. Ukunyuka kwe-Dose kusetyenziswa isakhiwo somveli "3 + 3" kunye neenkcazo eziqhelekileyo zobunyoyi bezilingo (DLT) kunye neqondo eliphezulu lokunyamezela.

③ Iziphumo
Kwizigulane ze-25 ababhalisile, ii-23 zavandlakanywa kwi-DLT kunye ne-17 zavavanywa ukuphendula. Inqanaba elixhasayo elixhasayo lidibeneyo yi-buparlisib 100 mg imihla ngemihla kunye ne-capecitabine 1000 mg / m2 kabini imihla ngemihla. I-DLTs ibandakanye ibanga le-3 hyperglycemia kunye ne-grade 3 ukudideka. Ibanga eliqhelekileyo le-3 isifo sohudo kunye nokuphakama kwe-aspartate aminotransferase kunye ne-alanine transaminase. Omnye isigulane wabonisa impendulo epheleleyo kwonyango kwaye ezine zineempendulo eziqinisekisiweyo. Kwi-coNts 3 kunye ne-4, apho i-dose ye-Buparlisib (944396-07-0) isoloko ihlala iqhubeka kodwa i-dose capecitabine yanda, ukwanda okwenziwe kwiinkcenkcesho ze-plasma zeplasmisi.

④ Isiphelo
Ukudibanisa i-buparlisib kunye ne-capecitabine kwizigulane ezineesifo somhlaza wesifo se-metastatic ngokuqhelekileyo sibekezelela, kunye nezigulane ezininzi zibonisa iimpendulo ezide. Amazinga angaphantsi angalindelekanga okutshintshwa kwe-PIK3CA (3 ye-17) yabonwa, kwaye kuphela i-2 ye-7 tumors kunye ne-subtyping yayiyi-luminal, okwenza ukuhlolisiswa kwala manqaku angabonakali. Uphando olongezelelweyo lwenxulumano alunangqiqo, kunye ne-pharmacokinetics eyandisiweyo kunye nokuhlalutya ngokulandelelwano ukuze kulungelelanise ngakumbi ukusebenzisana kweziyobisi kunye neziphumo zokuphendula ezichanekileyo.

I mi yalelo

Ukuguqulwa kwe-phosphatidylinositol i-3-kinase (PI3K) / i-AKT / i-mammalian injongo ye-rapamycin yokuyindlela yokumisela iyona nto ibalulekileyo ekukhuleni nasekusindekeni kwamanqamu amaninzi, kuquka nomhlaza wesifuba. Ukongezelela, ukutshatyalaliswa kwe-PI3K ukubonisa kungabangela ukuchasana namaqela amaninzi anticancer. I-PI3K inhibitors inokuthi isebenze njengonyango lwe-antineoplastic. I-Buparlisib yinto enamandla kakhulu kunye nomlomo othe ngqo kwi-inhibitor ye-pan-class I I-PI3K intsapho. I-Buparlisib igxininisa ngokukodwa itekisi I-PIK3 kwi-PI3K / AKT kinase indlela yokutshintshela ngendlela yokukhuphisana kwe-ATP, oko kukuvimbela ukuveliswa komthunywa wesibini we-phosphatidylinositol (3,4,5) -i-trisphosphate kunye nokusebenza kwe-PI3K indlela yokubonisa. Oku kunokubangela ukuvinjelwa kwe-cell tumor growth and survival in the tumor cell cell. I-Buparlisib okwangoku iphandwayo kwizigulane ezineentlobo ezahlukeneyo zesisu, kuquka nomhlaza wesifuba. I-Buparlisib iye yaqinisekiswa njengegosa elithembisa i-antiticancer, kwaye kwenziwa iinzame ezinkulu ukuphuhlisa. Nangona kunjalo, i-buparlisib monotherapy iye yabangela inzuzo ethobekileyo ngoku. Iziphumo ezivela kwizifundo ezidibanisa i-buparlisib kunye nama-agent anticancer ahlukeneyo-okuthi, unyango lwe-endocrine, unyango lwe-HER2, kunye ne-chemotherapy-lubonise ukuphumelela okungafaniyo kunye nefuthe elikhulu.


Indlela yokuthenga iBuparlisib ukusuka kwi-AASraw

1.Qhagamshelana nathi nge-imeyile yethu inkqubo yophando, okanye i-skype ye-intanethiummeli wenkonzo yamakhasimende (CSR).
2.Ukusibonelela ngobuninzi bakho kunye neadesi.
I-3.I-CSR yethu iya kukunika isingeniso, ixesha lokuhlawula, inombolo yokulandelela, iindlela zokuhambisa kunye nomhla wokufika oqikelelwayo (i-ETA).
I-4.Inkokhelo eyenziwe kwaye iimpahla ziya kuthunyelwa kwiiyure ze-12 (Ukuze ulandelwe ngaphakathi kwe-10kg).
5.Goods zifunyenwe kwaye zinike izimvo.

ISIQINISEKISO NESIBONELELO:

Le nto ithengiselwe uKwenziwa koPhando kuphela. Imigaqo yokuthengisa Faka isicelo. Ayisetyenziselwa uBuntu, okanye oNyango, iZilwanyana, okanye abaNtu.


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