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Sunitinib (CAS# 557795-19-4) Umfanekiso okhoyo
  • Suntinib (CAS# 557795-19-4) 1

Suntinib (CAS# 557795-19-4)

Ipropati yeMichiza:

Ifomula yeemolekyuli I-C22H27FN4O2
IMisa yeMolar 398.47
Ukuxinana 1.2
Indawo yokunyibilika 189-191°C
Indawo yeBoling 572.1±50.0 °C(Kuqikelelwe)
Indawo yokuflasha 299.8℃
Ukunyibilika 25°C: DMSO
Uxinzelelo loMphunga 3.13E-23mmHg ku-25°C
Imbonakalo Umgubo weCrystalline
Umbala Mthubi ukuya kwiOrenji emnyama
pKa 8.5(nge25℃)
Imeko yoGcino 2-8°C
MDL MFCD08273555
Isifundo se-in vitro I-Sunitinib iyasebenza ekunqandeni iKit kunye ne-FLT-3. I-Sunitinib yi-ATP esebenzayo yokuncintisana inhibitor ye-VEGFR2 (Flk1) kunye ne-PDGFRβ, i-KI yi-9 nM kunye ne-8 nM ngokulandelanayo, isebenza kwi-VEGFR2 kunye ne-PDGFR isebenza ngakumbi kune-FGFR-1, EGFR, Cdk2, Met,IGFR-1, Abl, kunye Ukhetho lwe-src lwalungaphezulu kwamaxesha ali-10 ngaphezulu. Kwiiseli ze-NIH-3T3 ezilambileyo ze-serum ezibonisa i-VEGFR2 okanye i-PDGFRβ, i-Sunitinib inhibithelwe i-VEGF-exhomekeke kwi-VEGFR2 phosphorylation kunye ne-PDGF-exhomekeke kwi-PDGFRβ phosphorylation kunye ne-IC50 ye-10 nM kunye ne-10 nM, ngokulandelanayo. Kwiiseli ze-NIH-3T3 ezigqithise ngokugqithiseleyo i-PDGFRβ okanye i-PDGFRα, i-Sunitinib inqanda ukwanda okubangelwa yi-VEGF kunye ne-IC50 ye-39 nM kunye ne-69 nM, ngokulandelanayo. I-Sunitinib inhibited wild-type FLT3,FLT3-ITD, kunye ne-FLT3-Asp835 phosphorylation kunye ne-IC50 ye-250 nM, i-50 nM, kunye ne-30 nM, ngokulandelanayo. I-Sunitinib ivimbele ukwanda kweeseli ze-MV4; i-11 kunye ne-OC1-AML5 kunye ne-IC50 ye-8 nM kunye ne-14 nM, ngokulandelanayo, kwaye ibangele i-apoptosis ngendlela exhomekeke kwidosi.
Kwisifundo se-vivo Ngokuhambelana nokuthintela okukhulu, okukhethiweyo kwe-phosphorylation kunye nokubonakaliswa kwe-VEGFR2 okanye i-PDGFR kwi-vivo, i-Sunitinib (20-80 mg / kg / ngosuku) ibonakaliswe inoxanduva lweemodeli ezahlukeneyo ze-tumor xenograft, kuquka i-HT-29, A431, Colo205, h. -460, SF763T,C6,A375, okanye I-MDA-MB-435 ibonise umsebenzi we-antitumor oxhomekeke kwidosi ngokubanzi. I-Sunitinib kwi-dose ye-80 mg / kg / ngosuku ngeentsuku ze-21 ibangele ukuguqulwa kwe-tumor epheleleyo kwi-6 yeegundane ze-8, kwaye ekupheleni kwonyango, i-tumor ayizange iphinde ihlaziywe ngexesha lokujonga iintsuku ze-110. Umjikelo wesibini wonyango nge-Sunitinib wawusasebenza ngokuchasene namathumba, kodwa awuzange uchache ngokupheleleyo kumjikelo wokuqala wonyango. Unyango lwe-Sunitinib lubangele ukuhla okukhulu kwi-tumor MVD, eyancitshiswa nge-~ 40% kwi-SF763T gliomas. Unyango lwe-SU11248 lubangele uthintelo olupheleleyo lokukhula kwe-tumor eyongezelelweyo ye-luciferase-ebonisa i-PC-3M xenografts, nangona kwakungekho kuncipha kobukhulu be-tumor. Kwimodeli yokutshintshwa kwamathambo e-FLT3-ITD, unyango lwe-Sunitinib (20 mg / kg / ngosuku) lunqande kakhulu ukukhula kwe-MV4;11 (FLT3-ITD) i-xenografts kunye nokuphila ixesha elide.

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Iithegi zeMveliso

Inkcazelo yoKhuseleko 24/25-Kuphephe ukudibana nolusu kunye namehlo.
Ikhowudi ye-HS 29337900

 

Intshayelelo

I-Sunitinib yi-RTK inhibitor ejoliswe kwizinto ezininzi ezijoliswe kuzo kwi-VEGFR2 (Flk-1) kunye ne-PDGFRβ kunye ne-IC50 ye-80 nM kunye ne-2 nM, kwaye inqanda i-c-Kit.

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