Sunitinib （CAS # 557795-19-4)

Umutungo wa Shimi:

Inzira ya molekulari	C22H27FN4O2
Misa	398.47
Ubucucike	1.2
Ingingo yo gushonga	189-191 ° C.
Ingingo ya Boling	572.1 ± 50.0 ° C (Biteganijwe)
Flash point	299.8 ℃
Gukemura	25 ° C: DMSO
Umwuka	3.13E-23mmHg kuri 25 ° C.
Kugaragara	Ifu ya Crystalline
Ibara	Umuhondo kugeza Umwijima
pKa	8.5 (kuri 25 ℃)
Imiterere y'Ububiko	2-8 ° C.
MDL	MFCD08273555
Mu bushakashatsi bwa vitro	Sunitinib ifite akamaro mukubuza Kit na FLT-3. Sunitinib ninzitizi nziza ya ATP irwanya VEGFR2 (Flk1) na PDGFRβ, KI ni 9 nM na 8 nM, gukina kuri VEGFR2 na PDGFR bifite akamaro kuruta FGFR-1, EGFR, Cdk2, Met, IGFR-1, Abl, na src guhitamo byari hejuru yikubye inshuro 10. Muri selile-inzara ya NIH-3T3 yerekana VEGFR2 cyangwa PDGFRβ, Sunitinib yabujije fosifora ya VEGFR2 iterwa na VEGFR2 hamwe na PDGFRβ iterwa na fosifori na IC50 ya 10 nM na 10 nM. Kuri selile NIH-3T3 ikabije PDGFRβ cyangwa PDGFRα, Sunitinib yabujije ikwirakwizwa ryatewe na VEGF hamwe na IC50 ya 39 nM na 69 nM. Sunitinib yabujije ubwoko bwa FLT3, FLT3-ITD, na fosifori ya FLT3-Asp835 hamwe na IC50 ya 250 nM, 50 nM, na 30 nM. Sunitinib yabujije ikwirakwizwa rya selile MV4; 11 na OC1-AML5 hamwe na IC50 ya 8 nM na 14 nM, kandi itera apoptose muburyo buterwa na dose.
Mu bushakashatsi bwa vivo	Bikwiranye no kubuza fosifora no kwerekana ibimenyetso bya VEGFR2 cyangwa PDGFR muri vivo, Sunitinib (20-80 mg / kg / kumunsi) byagaragaye ko ari yo nyirabayazana w’ibibyimba bitandukanye byerekana ibibyimba, harimo HT-29, A431, Colo205, h -460, SF763T, C6, A375, cyangwa MDA-MB-435 yerekanaga ibikorwa byinshi bya dose biterwa na antitumor. Sunitinib ku kigero cya 80 mg / kg / kumunsi iminsi 21 yatumye habaho gusubirana ibibyimba burundu muri 6 yimbeba 8, kandi nyuma yo kuvurwa, ibibyimba ntibyongeye kuvuka mugihe cyiminsi 110 yo kwitegereza. Icyiciro cya kabiri cyo kuvura hamwe na Sunitinib cyari kigifite akamaro mu kurwanya ibibyimba, ariko nticyakize neza mu cyiciro cya mbere cy’ubuvuzi. Kuvura Sunitinib byatumye igabanuka ryinshi rya MVD, ryagabanutseho ~ 40% muri glioma ya SF763T. Kuvura SU11248 byaviriyemo kubuza burundu ikibyimba cyiyongera cya luciferase yerekana PC-3M yerekana amashusho, nubwo nta kugabanya ubunini bwibibyimba. Mu buryo bwo guhinduranya amagufwa ya FLT3-ITD, kuvura Sunitinib (20 mg / kg / kumunsi) byabujije cyane imikurire ya MV4 yo munsi y'ubutaka; 11 (FLT3-ITD) ibishushanyo mbonera no kubaho igihe kirekire.