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Bosutinib（CAS# 380843-75-4) Ki‘i Mana‘o
  • Bosutinib（CAS# 380843-75-4) 1

Bosutinib（CAS# 380843-75-4)

Waiwai Kemika:

ʻĀpana Molekala C26H29Cl2N5O3
Molar Mass 530.45
ʻO ka mānoanoa 1.36
Lae hehee 116-120 ºC
Lae Boling 649.7±55.0 °C(Wānana ʻia)
Lae Flash 346.7°C
Ka hoʻoheheʻe Hiki ke hoʻoheheʻe ʻia i DMSO, ʻaʻole i ka wai
Puʻupuʻu mahu 0-0Pa ma 20 ℃
Ka nana aku Paʻa
kala kala keʻokeʻo keʻokeʻo i ka ʻeleʻele māmā
pKa 7.63±0.10(Wanamua)
Kūlana Waihona lumi lumi
Paʻa Paʻa no 2 mau makahiki mai ka lā i kūʻai ʻia e like me ka mea i hoʻolako ʻia. Hiki ke mālama ʻia nā hopena ma DMSO ma -20°C a hiki i ka mahina 1.
Hōʻike Hōʻike 1.651
Haʻawina in vitro Loaʻa i ka Bosutinib kahi koho kiʻekiʻe no Src ma mua o nā kinases ʻohana non-Src, me kahi IC50 o 1.2 nM, a hoʻopaʻa pono i ka hoʻonui ʻana o Src-dependent cell, me kahi IC50 o 100 nM. Ua kāohi nui ʻo Bosutinib i ka hoʻonui ʻana o nā laina cell leukemia Bcr-Abl-positive KU812, K562, a me MEG-01 akā ʻaʻole ʻo Molt-4, HL-60, Ramos, a me nā laina cell leukemia ʻē aʻe, me IC50 o 5 nM, 20 nM, kēlā me kēia. , a me 20 nM, ʻoi aku ka maikaʻi ma mua o STI-571. E like me STI-571, hana ʻo Bosutinib ma Abl-MLV hoʻololi i nā fibers a he hana proliferative me kahi IC50 o 90 nM. Ma ka nui o 50 nM, 10-25 nM, a me 200 nM, ua hoʻokuʻu ʻia ʻo Bosutinib i ka Bcr-Abl a me STAT5 i nā cell CML a me ka v-Abl tyrosine phosphorylation i hōʻike ʻia i loko o nā fibers, e hopena kēia i ka inhibition o ka phosphorylation o Bcr-Abl downstream hōʻailona Lyn. /Hck. ʻOiai ʻaʻole hiki ke kāohi i ka hoʻonui ʻana a me ke ola ʻana o nā maʻi kanesa o ka umauma, hiki ke hoʻemi nui i ka neʻe ʻana a me ka hoʻouka ʻana o nā maʻi kanesa o ka umauma, ʻo IC50 ka 250 nM, a hoʻomaikaʻi i ka adhesion intercellular a me ka localization membrane o β-catenin.
In vivo haʻawina Hoʻohana maikaʻi ʻo Bosutinib i nā ʻiole olohelohe e lawe ana i nā xenografts Src-transformed fiber a me HT29 xenografts ma kahi ʻano o 60 mg / kg i kēlā me kēia lā, me nā helu T / C o 18% a me 30%, kēlā me kēia. ʻO ka lawelawe waha o Bosutinib i nāʻiole no nā lā 5 i kāohi nui i ka uluʻana o nā maʻi maʻi K562 ma kahiʻano hilinaʻi. Ua hoʻopau ʻia nā ʻōpū nui ma kahi ʻano o 100 mg / kg, mālama ʻia ma kahi ʻano o 150 mg / kg i wehe ʻia i nā ʻōpū me ka ʻole o ka ʻawaʻawa. Ke hoʻohālikelike ʻia me ka hopena ma ka HT29 transplanted tumor, ʻo Bosutinib ma kahi ʻano o 75 mg / kg, ʻelua ʻelua i ka lā, hiki ke kāohi i ka ulu ʻana o ka maʻi maʻi i nā ʻiole olohelohe e lawe ana i ka maʻi ʻo Colo205 transplanted tumor, ʻaʻohe hopena kiʻekiʻe ma hope o ka hoʻonui ʻana i ka nui, akā ʻo ka 50 mg/ ʻAʻole i loaʻa ka hopena o ka dose kg.

Huahana Huahana

Huahana Huahana

Nā hōʻailona pōʻino Xi – Hoʻohaunaele
Nā Code Risk 36 - Hoʻonāukiuki i nā maka
Ka wehewehe palekana 26 - Inā pili me nā maka, holoi koke me ka wai nui a ʻimi i ka ʻōlelo aʻoaʻo olakino.
WGK Kelemānia 3
HS Code 29335990

 

Hoʻolauna

ʻO Bosutinib kahi mea paʻa pālua o Src / Abl me IC50 o 1.2 nM a me 1 nM, kēlā me kēia.

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