84573-16-0
84573-16-0 結(jié)構(gòu)式
基本信息
洛克米蘭酰胺
(1R,2R,3S,3AR,8BS)-1,8B-二羥基-6,8-二甲氧基-3A-(4-甲氧基苯基)-N,N-二甲基-3-苯基-2,3,3A,8B-四氫-1H-環(huán)戊二烯并[B]苯并呋喃-2-甲酰胺
NSC 326408
ROCAGLAMIDE
Rocaglamide A
N,N-Dimethyl-1α,8bβ-dihydroxy-6,8-dimethoxy-3β-phenyl-3aβ-(4-methoxyphenyl)-2,3,3a,8b-tetrahydro-1H-cyclopenta[b]benzofuran-2α-carboxamide
2,3,3a,8b-Tetrahydro-N,N-dimethyl-1α,8bβ-dihydroxy-6,8-dimethoxy-3β-phenyl-3aβ-(4-methoxyphenyl)-1H-cyclopenta[b]benzofuran-2α-carboxamide
2,3,3a,8b-Tetrahydro-1α,8bβ-dihydroxy-6,8-dimethoxy-3aβ-(4-methoxyphenyl)-N,N-dimethyl-3β-phenyl-1H-cyclopenta[b]benzofuran-2α-carboxamide
(1R)-N,N-Dimethyl-1α,8bβ-dihydroxy-3β-phenyl-3aβ-(4-methoxyphenyl)-6,8-dimethoxy-2,3,3a,8b-tetrahydro-1H-cyclopenta[b]benzofuran-2α-carboxamide
(1R)-2,3,3a,8b-Tetrahydro-1α,8bβ-dihydroxy-6,8-dimethoxy-3aβ-(4-methoxyphenyl)-N,N-dimethyl-3β-phenyl-1H-cyclopenta[b]benzofuran-2α-carboxamide
(1R,2R,3S,3aR,8bS)-2,3,3a,8b-Tetrahydro-1,8b-dihydroxy-6,8-dimethoxy-3a-(4-methoxyphenyl)-N,N-dimethyl-3-phenyl-1H-cyclopenta[b]benzofuran-2-carboxamide
物理化學(xué)性質(zhì)
常見(jiàn)問(wèn)題列表
(2) 楝酰胺的直接作用靶標(biāo)為ULK1，ULK1是參與自噬發(fā)生的重要激酶。
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HSF1 50 nM (IC 50 ) |
Rocaglamide enhances TRAIL-induced apoptosis in resistant HCC cells. Treatment with Rocaglamide alone leads to apoptosis in 9% HepG2 and 11% Huh-7 cells and treatment with TRAIL induces apoptosis in 16% HepG2 and 17% Huh-7 cells. However, the combination of Rocaglamide and TRAIL induces apoptosis in 55% HepG2 and 57% Huh-7 cells, which is evidently more than an additive effect. A similar result is obtained by measurement of cell viability using crystal violet staining. Rocaglamide has the potential to sensitize highly chemoresistant HepG2 and Huh-7 cells to TRAIL-based therapy.
Tumor volumes in the Rocaglamide-treated group are 45±12% compared with the control group. Rocaglamide significantly suppresses tumor growth compared with that in the control group. Treatment with Rocaglamide does not lead to any reduction in body weight and no apparent signs of toxicity are observed in the mice during the treatment, suggesting that Rocaglamide is generally tolerated well.