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Buparlisib (944396-07-0)

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5.00 tawm ntawm 5 raws li nyob rau 1 neeg ntsuam xyuas
SKU: 944396-07-0. Qeb:

AASraw yog nrog synthesis thiab muaj peev xwm ua tau los ntawm cov gram kom loj npaum li cas ntawm Buparlisib (CAS 944396-07-0), raws li CGMP cov kev tswj thiab kev tswj xyuas qhov kev tswj kom zoo.

Buparlisib hmoov yog ib lub qhov ncauj, tsis meej, meej meej, thiab muaj zog ntawm tus iav hauv tsev phomphatidylinositol 3-kinase (PI3K) tsev neeg, thiab nws lub luag haujlwm tam li ib tus neeg sawv cev ntawm chaw ua haujlwm yog tam sim no nyob rau hauv kev tshawb xyuas.

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Buparlisib video


Buparlisib tus cwj pwm yooj yim

Lub npe: Buparlisib
CAS: 944396-07-0
Molecular Formula: C18H21F3N6O2
Molecular phaus: 410.3935496
Melt Point: 645.7 ± 65.0 ° C
Cia Temp: -20 ° C
xim: Dawb crystalline hmoov


Buparlisib (944396-07-0) kev siv nyob rau hauv kev hloov tho txawv

npe

Buparlisib (944396-07-0), ib lub qhov ncauj-chav kawm I phosphotidyinositol-3-kinase (PI3K) inhibitor.

Kev Kuaj Mob Cancer Mis

① Background

Buparlisib yog ib lub tsho lub hauv paus I phosphotidyinositol-3-kinase (PI3K) inhibitor. Tam sim no theem kuv kawm ntsuam xyuas txoj kev nyab xeeb, tshuaj khomob, thiab ua haujlwm ntawm buparlisib nrog capecitabine rau cov neeg mob uas muaj mob cancer mis.

② Tus neeg mob thiab txoj kev
Cov neeg mob tau txais buparlisib ib zaug txhua hnub (ntau yam, 50 rau 100 mg) rau 3 lub lis piam nrog capecitabine ib hnub ob zaug (ntau yam, 1000 rau 1250 mg / m2) rau 2 lub lis piam nrog kev xiam 1. Dose escalation siv ib txwm "3 + 3" tsim nrog kev txhais cov ntsiab lus ntawm koob tshuaj-limiting toxicity (DLT) thiab cov tshuaj tiv thaiv siab tshaj plaws.

③ Cov ntsiab lus
Ntawm 25 cov neeg mob npe, 23 tau ntsuam xyuas rau DLT thiab 17 tau ntsuam xyuas rau cov lus teb. Tshaj siab tshaj plaws ntawm kev sib tiv ntawm kev ua ke yog buparlisib 100 mg txhua txhua hnub thiab capecitabine 1000 mg / m2 ob zaug ib hnub. DLTs muaj qib 3 hyperglycemia thiab qib 3 tsis meej pem. Qib siab tshaj plaws hauv 3 toxicities yog mob raws plab thiab nce qib ntawm aspartate aminotransferase thiab thaj tsam transaminase. Ib tus neeg mob tau teb ib qho kev kho mob kom tiav thiab plaub leeg tau lees paub ib nrab. Hauv kev sib koom tes 3 thiab 4, uas cov Buparlisib (944396-07-0) koob tshaj plaws tab sis qhov capecitabine koob twb nce lawm, tseem ceeb ntxiv hauv cov buparlisib plasma concentration tau sau tseg.

④ xaus
Ua ke nrog ntawm buparlisib nrog capecitabine rau cov neeg mob mob metastatic mis mob cancer feem ntau zoo-tolerated, nrog rau ntau cov neeg mob qhia cov lus teb ntev. Tshaj poob qis ntawm PIK3CA mutations (3 ntawm 17) tau pom, thiab 2 7 qog nrog subtyping muaj luminal, kev tshawb nrhiav ntawm cov kev txwv tias yuav ua kom tsis muaj kev txwv. Cov kev tshawb fawb ntxiv ntawm kev ua ke tsis yog tsis tsim nyog, nrog cov tshuaj pharmacokinetics thiab cov txheej txheem sib hloov kom zoo dua tuaj yeem paub cov kev siv tshuaj yeeb-tshuaj thiab ntau qhov tseeb ntawm cov lus teb.

Cov lus qhia ntxiv

Kev hloov ntawm phosphatidylinositol 3-kinase (PI3K) / AKT / mammalian lub hom phiaj ntawm qhov tsom mus rau qhov chaw kho mob yog qhov tseem ceeb rau kev loj hlob thiab ciaj sia taus ntawm ntau cov qog nqaij hlav, nrog rau kev mob qog mis. Tsis tas li, Dysregulation ntawm PI3K signaling yuav ua rau muaj kev tiv thaiv rau ntau tus neeg siv tshuaj tua kabmob. PI3K inhibitors yuav ua rau, yog li ntawd, ua zoo li cov tshuaj tiv thaiv antineoplastic. Buparlisib yog ib qho muaj zog thiab meej tshwj xeeb ntawm lub qhov ncauj ntawm lub iav-chav kawm ntawv kuv PI3K tsev neeg. Buparlisib uas yog chav kawm PIK3 hauv PI3K / AKT kinase signaling pathway hauv ATP-kev sib tw, yog li inhibiting qhov kev tshaj tawm tub ceev xwm phosphatidylinositol (3,4,5) -phisphosphate thiab ua rau PI3K signaling pathway. Qhov no yuav ua rau kom muaj kev tiv thaiv ntawm cov qog cell loj hlob thiab ciaj sia taus nyob rau hauv cov nqaij mob nyhuv. Buparlisib yog tam sim no nyob rau hauv kev tshawb nrhiav nyob rau hauv cov neeg mob uas muaj ntau yam khoom hlav, nrog rau kev mob qog mis. Buparlisib tau lees paub tias yog ib tus neeg sawv cev pheej cia siab, thiab muaj kev sib zog ua haujlwm tau tsim los tsim nws. Txawm li cas los, buparlisib monotherapy tau ua rau txo hwj chim pab kom deb li deb. Ntawm cov kev tshawb fawb sib koom ua ke buparlisib nrog cov neeg txawv txawv cov neeg muag tshuaj - namely, endocrine therapy, anti-HER2 kev kho, thiab kws khomob - muaj kev pom tau tias cov txiaj ntsig zoo sib xws nrog kev muaj cov tshuaj muaj ntau.


Yuav ua li cas yuav Buparlisib los ntawm AASraw

1.To tiv tauj peb ntawm peb tus email nug qhov system, lossis hauv internettus sawv cev rau tus neeg sawv cev (CSR).
2.To muab peb nug koj qhov ntau thiab qhov chaw nyob.
3.Our CSR yuav muab nqe lus hais txog koj, qhov them nqi, tus lej nrhiav, kev xaib thiab kwv yees hnub uas tuaj txog (ETA).
4.Payment ua tiav thiab cov khoom xa tuaj rau 12 cov xuab moos (Rau kev txiav txim hauv 10kg).
5.Goods tau txais thiab muab tswv yim.

PRECAUTION THIAB DISCLAIMER:

Cov Khoom Siv No Yog Muag Rau Kev Tshawb Xyuas Siv Xwb. Cov ntsiab lus ntawm kev muag khoom Thov. Tsis Yog Rau Tib Neeg Noj, Tsis Kho Mob, Kho Tsiaj, lossis Tsev Neeg Siv.


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COA

HNMR

Zaub mov txawv

References & cov khoom citations