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453562-69-1

中文名稱 莫特塞尼
英文名稱 Motesanib
CAS 453562-69-1
分子式 C22H23N5O
分子量 373.45
MOL 文件 453562-69-1.mol
更新日期 2024/12/17 14:15:52
453562-69-1 結(jié)構(gòu)式 453562-69-1 結(jié)構(gòu)式

基本信息

中文別名
莫替沙尼
莫特塞尼
莫特沙芬
莫桑尼布雜質(zhì)
莫替沙尼、莫替沙尼
莫特塞尼,莫替沙尼
VEGFR1/VEGFR2/VEGFR3抑制劑(MOTESANIB)
N-(2,3-二氫-3,3-二甲基-1H-吲哚-6-基)-2-[(4-吡啶甲基)氨基]-3-吡啶甲酰胺
3-吡啶甲酰胺, N-(2,3-二氫-3,3-二甲基-1H-吲哚-6-基)-2-[(4-吡啶基甲基)氨基]-
英文別名
D06678
CS-1108
motesanib
Motesanib Base
AMG 706
AMG-706
AMG-706(Motesanib)
Motesanib (AMG-706) Base)
N-(3,3-dimethylindolin-6-yl)-2-(pyridin-4-ylmethylamino)nicotinamide
N-(3,3-dimethylindolin-6-yl)-2-(pyridin-4-ylmethylamino)nicotinamide,AMG706
N-(3,3-diMethylindolin-6-yl){2-[(4-pyridylMethyl)-aMino](3-pyridyl)}-carboxaMide
所屬類別
生物化工:激動(dòng)劑抑制劑

物理化學(xué)性質(zhì)

熔點(diǎn)147-150°C
沸點(diǎn)517.3±50.0 °C(Predicted)
密度1.251
儲(chǔ)存條件Refrigerator
溶解度可溶于DMSO(少許)、甲醇(少許)
酸度系數(shù)(pKa)11.75±0.40(Predicted)
形態(tài)白色粉末狀固體。
顏色淡黃色

安全數(shù)據(jù)

危險(xiǎn)性符號(hào)(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險(xiǎn)性描述H315-H319-H335
海關(guān)編碼2933399990

常見問(wèn)題列表

簡(jiǎn)介
Motesanib 是一種有效的 VEGFR1/2/3 的 ATP 競(jìng)爭(zhēng)性抑制劑,IC50 值為 2 nM/3 nM/6 nM,與對(duì)Kit的選擇性相似,是 PDGFR 和 Ret的 10 倍多。
用途

莫特塞尼,也稱為AMG-706,是一種多激酶抑制劑,可選擇性靶向VEGF受體,血小板源性生長(zhǎng)因子受體(PDGFRs)和Kit受體,IC??值分別為2 nM(VEGFR1),3 nM(VEGFR2),6 nM (VEGFR3),84 nM(PDGFR)和8 nM(Kit)。 它也有效地抑制了血管生成并誘導(dǎo)了異種腫瘤的消退。

用途
莫特塞尼是一種Flk-1、Flt-4、PDGFR-和c-Kit的抑制劑。
生物活性
Motesanib (AMG-706)是一種具有口服生物活性的受體酪氨酸激酶 (receptor tyrosine kinase)抑制劑,對(duì)VEGFR1, VEGFR2, VEGFR3, Kit, PDGFR和Ret的IC50值分別為2、3、6、8、84和59 nM。
靶點(diǎn)
TargetValue
VEGFR1
(Cell-free assay)
2 nM
VEGFR2
(Cell-free assay)
3 nM
VEGFR3
(Cell-free assay)
6 nM
c-Kit
(Cell-free assay)
8 nM
c-Kit
(Cell-free assay)
8 nM
體外研究

Motesanib has broad activity against the human VEGFR family, and displays > 1000 selectivity against EGFR, Src, and p38 kinase. Motesanib significantly inhibits VEGF-induced cellular proliferation of HUVECs with an IC 50 of 10 nM, while displaying little effect at bFGF-induced proliferation with an IC 50 of >3,000 nM. Motesanib also potently inhibits PDGF-induced proliferation and SCF-induced c-kit phosphorylation with IC 50 of 207 nM and 37 nM, respectively, but not effective against the EGF-induced EGFR phosphorylation and cell viability of A431 cells.?Althouth displaying little antiproliferative activity on cell growth of HUVECs alone, Motesanib treatment significantly sensitizes the cells to fractionated radiation.

體內(nèi)研究

Motesanib (100 mg/kg) significantly inhibits VEGF-induced vascular permeability in a time-dependent manner. Oral administration of Motesanib twice daily or once daily potently inhibits, in a dose-dependent manner, VEGF-induced angiogenesis using the rat corneal model with ED 50 of 2.1 mg/kg and 4.9 mg/kg, respectively. Motesanib induces a dose-dependent tumor regression of established A431 xenografts by selectively targeting neovascularization in tumor cells. Motesanib in combination with radiation displays significant anti-tumor activity in head and neck squamous cell carcinoma (HNSCC) xenograft models.?Motesanib treatment also induces significant dose-dependent reductions in tumor growth and blood vessel density of MCF-7, MDA-MB-231, or Cal-51 xenografts, which can be markedly enhanced when combined with docetaxel or tamoxifen.

莫特塞尼價(jià)格(試劑級(jí))
報(bào)價(jià)日期產(chǎn)品編號(hào)產(chǎn)品名稱CAS號(hào)包裝價(jià)格
2024/11/08HY-10228莫特塞尼
Motesanib
453562-69-15mg540元
2024/11/08HY-10228莫特塞尼
Motesanib
453562-69-110mM * 1mLin DMSO600元
2024/11/08HY-10228莫特塞尼
Motesanib
453562-69-110mg650元
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