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286936-40-1

中文名稱 OTX008
英文名稱 OTX 008
CAS 286936-40-1
分子式 C52H72N8O8
分子量 937.18
MOL 文件 286936-40-1.mol
更新日期 2026/05/20 17:05:55
286936-40-1 結(jié)構(gòu)式 286936-40-1 結(jié)構(gòu)式

基本信息

中文別名
化合物OTX008
2,2',2'',2'''-(1,3,5,7(1,3)-四苯環(huán)辛烷-12,32,52,72-四基四(氧基))四(N-(2-(二甲基氨基)乙基)乙酰胺)
英文別名
PTX 008
Calixarene 0118
OTX008 (Calixarene 0118
Calix[4]arene compound 0118
OTX008 (Synonyms: Calixarene 0118
Acetamide, 2,2',2'',2'''-[pentacyclo[19.3.1.13,7.19,13.115,19]octacosa-1(25),3,5,7(28),9,11,13(27),15,17,19(26),21,23-dodecaene-25,26,27,28-tetrayltetrakis(oxy)]tetrakis[N-[2-(dimethylamino)ethyl]-

物理化學(xué)性質(zhì)

沸點(diǎn)1143.4±65.0 °C(Predicted)
密度1.155±0.06 g/cm3(Predicted)
儲(chǔ)存條件-20°C儲(chǔ)存
溶解度DMF: 1 mg/ml; DMSO: 2 mg/ml; Ethanol: 5 mg/ml; PBS (pH 7.2): 0.5 mg/ml
酸度系數(shù)(pKa)13.84±0.46(Predicted)
形態(tài)結(jié)晶固體
顏色White to off-white

圖譜信息

OTX008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
2026/03/03S6949OTX008
OTX008
286936-40-15mg1941.21元
2026/03/03S6949OTX008
OTX008
286936-40-125mg5872.45元

常見問題列表

生物活性
OTX008 (Calixarene 0118, PTX008) 一種杯芳烴衍生物,是 galectin-1 (Gal1) 的選擇性抑制劑,具有抗腫瘤活性。
靶點(diǎn)
TargetValue
galectin-1
()
體外研究

Growth inhibitory concentrations (GI 50 ) of OTX008 in a large panel of human solid tumour cell lines ranges from 3 to 500 μM. A significant correlation between OTX008 GI 50 values and Gal1 mRNA (LGALS1) and protein expression levels in the panel of cancer cells is observed. In SQ20B and A2780-1A9 cells, OTX008 inhibits Gal1 expression and ERK1/2 and AKT-dependent survival pathways, and induces G2/M cell cycle arrest through CDK1. OTX008 enhances the anti-proliferative effects of Semaphorin-3A (Sema3A) in SQ20B cells and reverses invasion induced by exogenous Gal1. OTX008 affects endothelial cell proliferation, motility, invasiveness, and cord formation. Tumor cell proliferation is also inhibited, with differences in sensitivity among cell lines (IC 50 from 1 to 190 μM).

體內(nèi)研究

OTX008 inhibits growth of A2780-1A9 xenografts. OTX008 treatment is associated with down-regulation of Gal1 and Ki67 in treated tumours, as well as decreased microvessel density and VEGFR2 expression. Finally, combination studies show OTX008 synergy with several cytotoxic and targeted therapies, principally when OTX008 is administered first.

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