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124689-65-2

中文名稱 CS-1374
CAS 124689-65-2
分子式 C35H43ClN2O8
分子量 655.18
124689-65-2 結(jié)構(gòu)式 124689-65-2 結(jié)構(gòu)式

基本信息

英文別名
CS-1374
Cryptophycin
cryptophycin 1
Cyclo[(2R)-2-methyl-β-alanyl-(2S)-2-hydroxy-4-methylpentanoyl-(2E,5S,6S)-5-hydroxy-6-[(2R,3R)-3-phenyl-2-oxiranyl]-2-heptenoyl-3-chloro-O-methyl-D-tyrosyl]

物理化學(xué)性質(zhì)

比旋光度White or light colored glassy solid. D +33.8° (c = 1.83 in methanol)

安全數(shù)據(jù)

危險品運輸編號3172
危險等級6.1(b)
包裝類別III

常見問題列表

生物活性
Cryptophycin 1 是一種從 Nostoc sp. 中分離出來的有效的細胞毒性抗微管劑。Cryptophycin 1 可以誘導(dǎo)細胞凋亡,并具有抗腫瘤活性和出色的抗增殖能力。
體外研究

Cryptophycin 1 (50 pM) rapidly causes morphological changes consistent with the induction of apoptosis in SKOV3 and MDA-MB-435 cells.
Cryptophycin 1 (50 pM; 12-24 h) causes an accumulation of MDA-MB-435 cells in G2/M.
Cryptophycin 1 (100 nM; 1-7 min) markedly reduces the rates and extents of microtubule shortening and growing events and dramatically increases the duration of phases of attenuation or pause.

Apoptosis Analysis

Cell Line: SKOV3 cells
Concentration: 50 pM
Incubation Time: 4 hours
Result: Caused rapid cell shrinkage, loss of the normal elliptical spheroid shape and the formation of membrane blebs.

Cell Cycle Analysis

Cell Line: MDA-MB-435 cells
Concentration: 50 pM
Incubation Time: 12, 18, 24 hours
Result: A doubling in the number of cells in G 2 /M at 12 hr.
Still a large number of cells (58%) in G 2 /M at 18 hr.
體內(nèi)研究

Cryptophycin 1 (i.v.) exhibits anti-tumor activity in mice.

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