142861-00-5
142861-00-5 結(jié)構(gòu)式
基本信息
中文別名
除草二烯 英文別名
GEX1ATAN-1609
Herboxidiene
2-((2R,5S,6S)-6-((S,2E,4E)-7-((2R,3R)-3-((2R,3R,4R)-4-hydroxy-3-methoxypentan-2-yl)-2-methyloxiran-2-yl)-6-methylhepta-2,4-dien-2-yl)-5-methyltetrahydro-2H-pyran-2-yl)acetic acid
L-glycero-L-gluco-Heptitol, 5,6-anhydro-6-C-[(2S,3E,5E)-6-[(2S,3S,6R)-6-(carboxymethyl)tetrahydro-3-methyl-2H-pyran-2-yl]-2-methyl-3,5-heptadien-1-yl]-1,4,7-trideoxy-4-methyl-3-O-methyl-
物理化學(xué)性質(zhì)
沸點(diǎn)567.9±35.0 °C(Predicted)
密度1.056±0.06 g/cm3(Predicted)
儲(chǔ)存條件-20°C
溶解度溶于DMSO或乙醇
酸度系數(shù)(pKa)4.38±0.10(Predicted)
形態(tài)固體
顏色白色
穩(wěn)定性Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.
LogP3.459 (est)
常見(jiàn)問(wèn)題列表
生物活性
Herboxidiene (GEX1A) 是一種有效的植物毒性聚酮類化合物，來(lái)源于鏈霉菌 A7847，具有多種活性，包括除草、抗膽固醇、抗腫瘤等。Herboxidiene 通過(guò)與剪接體相關(guān)蛋白 (SAP) 155 結(jié)合抑制前 mRNA 剪接 (pre-mRNA splicing) 過(guò)程，SAP 是剪接體中 SF3b 的一個(gè)亞單位。體外研究
Herboxidiene (24 hours) induces both G1 and G2/M arrest in a human normal fibroblast cell line, WI-38, with an IC
50
of 7.6 nM.
Herboxidiene exhibits cytotoxicity against A431, A549, and DLD-1 cells with IC
50
s of 3.7, 21, 51 nM, respectively.
體內(nèi)研究
Herboxidiene (GEX1A) (1 mg/kg; i.p.; once) shows significant antitumor activity.
| Animal Model: | BALB/c mice (bearing SVT2 murine fibrosarcoma) |
| Dosage: | 1 mg/kg |
| Administration: | I.p.; once |
| Result: | Showed significant antitumor activity on day 4. |