DIDESMETHYLROCAGLAMIDE

生物活性靶点体外研究 DIDESMETHYLROCAGLAMIDE 试剂级价格

CAS号:177262-30-5
英文名:1H-Cyclopenta[b]benzofuran-2-carboxamide, 2,3,3a,8b-tetrahydro-1,8b-dihydroxy-6,8-dimethoxy-3a-(4-methoxyphenyl)-3-phenyl-, (1R,2R,3S,3aR,8bS)-
中文名:DIDESMETHYLROCAGLAMIDE
CBNumber:CB38108051
分子式:C27H27NO7
分子量:477.51
MOL File:177262-30-5.mol

DIDESMETHYLROCAGLAMIDE化学性质

沸点 :691.4±55.0 °C(Predicted)
密度 :1.379±0.06 g/cm3(Predicted)
储存条件 :Store at -20°C
溶解度 :DMSO: 100 mg/mL (209.42 mM)
形态 :Solid
酸度系数(pKa) :11.70±0.70(Predicted)
颜色 :White to off-white

DIDESMETHYLROCAGLAMIDE性质、用途与生产工艺

生物活性 Didesmethylrocaglamide 是一种 Rocaglamide 的衍生物，也是一种有效的真核起始因子 4A (eIF4A) 抑制剂。Didesmethylrocaglamide 具有有效的生长抑制活性，IC50 为 5 nM。Didesmethylrocaglamide 抑制多种促进生长的信号通路，并诱导肿瘤细胞凋亡 (apoptosis)。抗肿瘤活性。
靶点

Eukaryotic initiation factor 4A (eIF4A)

体外研究

Didesmethylrocaglamide (5 nM, and 10 nM; 72 hours; MPNST cells) treatment arrests MPNST cells at G2-M, increases the sub-G1 population, induces cleavage of caspases and PARP, and elevates the levels of the DNA-damage response marker γH2A.X, while decreasing the expression of AKT and ERK1/2.
Didesmethylrocaglamide inhibits MPNST cell proliferation by inducing cell cycle arrest at G2/M and subsequently, cell death. Didesmethylrocaglamide-treated 697-R cells exhibits IC ₅₀ values is very similar to those of parental 697 cells (4 vs 3nM of IC ₅₀ , respectively).
Didesmethylrocaglamide induces apoptosis in both neurofibromatosis type 1 (NF1)-expressing and NF1-deficient MPNST cells, possibly subsequent to the activation of the DNA damage response. Didesmethylrocaglamide-treated sarcoma cells show decreased levels of multiple oncogenic kinases, including insulin-like growth factor-1 receptor.

Western Blot Analysis

Cell Line:	Malignant peripheral nerve sheath tumors (MPNST) cells
Concentration:	5 nM, and 10 nM
Incubation Time:	72 hours
Result:	Induced cleavage of caspases and PARP, and elevated the levels of the DNA-damage response marker γH2A.X.