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Buparlisib (944396-07-0)

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SKU: 944396-07-0. Category:

MUTSVENE unobatsira nekugadzira zvigadzirwa kubva ku gram kusvika kuhutano hweBuparlisib (CAS 944396-07-0), pasi peCGMP mutemo uye nehutsika hwehutano hwekutonga.

Buparlisib powder inonyorwa, isina kuwanikwa, yakanyatsotsanangurwa, uye yakasimba inhibitor ye pan-class I phosphatidylinositol 3-kinase (PI3K) yemhuri, uye basa rayo rinogona kuitwa senhengo yekare inoparidzirwa iye zvino iri kuongorora.

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Product Description

Buparlisib video


Buparlisib basic Characters

Name: Buparlisib
CAS: 944396-07-0
Molecular Formula: C18H21F3N6O2
Molecular Weight: 410.3935496
Melt Point: 645.7 ± 65.0 ° C
Storage Temp: -20 ° C
Color: White crystalline powder


Buparlisib (944396-07-0) kushandiswa mu-steroid cycle

Mazita

Buparlisib (944396-07-0), gorosi rinowanikwa mumuromo I phosphotidyinositol-3-kinase (PI3K) inhibitor.

Clinical Breast Cancer

① kureva

Buparlisib inhengo yepan-class I phosphotidyinositol-3-kinase (PI3K) inhibitor. Chikamu chazvino chandinoongorora ndechokuongorora kuchengetedzwa, pharmacokinetics, nekubudirira kweBuparlisib ne capecitabine kune varwere vane kenza yematenda emuviri.

② Mushonga uye Nzira
Varwere vakagamuchira buparlisib kamwe zuva nezuva (kureba, 50 kusvika ku100 mg) kwevhiki dze3 dzine capecitabine kaviri zuva nezuva (kureba, 1000 kusvika 1250 mg / m2) kwevhiki dze2 dzine 1-vhiki yevhiki. Dose escalation yakashandisa mutsika "3 + 3" yakagadziriswa nemashoko akazara ekurasikirwa kwechirwere (DLT) uye chiremba chakanyanya kubvumirwa.

③ zvitsva
Pakati pevarwere ve25 vakanyoresa, 23 yakaongororwa neDLT uye 17 yakaongororwa pamhinduro. Nhamba yakawanda yakanyatsoraramika yekusanganiswa yaiva buparlisib 100 mg zuva nezuva uye capecitabine 1000 mg / m2 kaviri zuva rimwe nerimwe. DLTs inosanganisira grade 3 hyperglycemia uye grade 3 kuvhiringidzika. Yakawanda yegadhesi 3 toxicities yaiva chirwere uye kukwira kweApartate aminotransferase uye alanine transaminase. Mumwe murwere akaratidza kupindura kwakakwana kurapwa uye mana aiva nemhinduro yakasarudzwa. Mumakwikwi 3 uye 4, umo Buparlisib (944396-07-0) dose yakaramba iripo asi maitiro e-capecitabine akawedzerwa, kuwedzerwa kukuru mukutarisa kweparparlisib plasma kwakaonekwa.

④ Kugumisa
Kubatanidzwa kweBuparlisib ne Capecitabine muvarwere vane kenza yemasasa inowanzoita zvakanaka, pamwe nevarwere vanoverengeka vachiratidza mhinduro refu. Zvisingatarisirwi zvakadzika pasi zvePIK3CA mutations (3 ye17) zvakaonekwa, uye chete 2 yezvipumbwe zve7 nekutengesa kwaiva chiedza, zvichiita kuti kuongororwa kweiyi putative predictive markers isabviri. Kuwedzera kumwe kudzidza kwekubatanidzwa hakusi kwepfungwa, nekuwedzera pharmacokinetics uye kuongororwa kwekutsvaga kuti zvive nani kujekesa kushandiswa kwezvinodhaka-zvinodhaka uye kunyanya kushandiswa kwezvakaitika zvehupenyu hwekupindura.

Mamwe mirayiridzo

Kugadziriswa kwephosphatidylinositol 3-kinase (PI3K) / AKT / mammalian chinangwa che rapamycin chinoratidza nzira yekukura uye kupona kwekenza dzakawanda, kusanganisira kenza yemazamu. Mukuwedzera, kuderedzwa kwePI3K kujekesa kunogona kubatsira mukurwisa maverengani anticancer agents. PI3K inhibitor, saka, inoshanda seine antineoplastic therapy. Buparlisib inonyanya uye yakanyatsonaka muromo inhibitor wepas-class I PI3K mhuri. Buparlisib inonyanya inhibits kirasi I PIK3 muPI3K / AKT kinase kugonesa nzira munzira yeCPP-inokwikwidza, nokudaro kudzivisa kubudiswa kwechipiri mutumwa phosphatidylinositol (3,4,5) -trisphosphate uye kushandiswa kwePI3K nzira yekucherechedza. Izvi zvinogona kukonzera kusagadzikana kwechiremera chekukura kwekukura uye kupona kunotora tumor cell cell. Buparlisib iye zvino ari pasi pekuongororwa nevarwere vane marudzi akasiyana-siyana emakumbo akakura, kusanganisira kenza yemvere. Buparlisib yakagadziriswa sechivimbiso chechirwere chekare, uye miitiro yakawanda yakatorwa kuti irikure. Zvisinei, buparlisib monotherapy yakaguma nokuzvininipisa zvishoma kusvika zvino. Migumisiro kubva kuongororo inobatanidza buparlisib neanticancer-agents dzakasiyana-siyana, kureva, endocrine therapy, anti-HER2 therapy, uye chemotherapy - dzakaratidza kushandiswa kushandiswa nehuwandu hwehuwandu hwekutyisa.


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