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459-86-9

中文名稱 丙脒腙
英文名稱 Mitoguazone
CAS 459-86-9
分子式 C5H12N8
分子量 184.2
MOL 文件 459-86-9.mol
459-86-9 結(jié)構(gòu)式 459-86-9 結(jié)構(gòu)式

基本信息

中文別名
米托瓜酮
丙雙脒腙
丙酮雙脒腙
米托胍腙(又名鹽酸丙脒腙)
英文別名
MGBG
Me-GAG
methyl-g
methyl-gag
Mitoguazone USP/EP/BP
Mitoguazone(Methyl-GAG)
Methylglycoxali BisguanylhydrazonuM
Pyruvaldehyde bis(amidinohydrazone)
1,1'-((methylethanediylidene)dinitrilo)diguanidine
1,1'-((methylethanediylidene)dinitrilo)di-guanidin
所屬類別
化學(xué)試劑:腙

物理化學(xué)性質(zhì)

外觀性狀白色結(jié)晶,熔點(diǎn)256-257℃(分解)。極易溶于水,在酸性水中較穩(wěn)定,在堿性介質(zhì)中不穩(wěn)定。
熔點(diǎn)225 °C (decomp)
沸點(diǎn)323.8±25.0 °C(Predicted)
密度1.55±0.1 g/cm3(Predicted)
儲(chǔ)存條件-20°C儲(chǔ)存
酸度系數(shù)(pKa)7.63, 9.05(at 25℃)
形態(tài)Solid
顏色Light brown to brown
水溶解性Water: 50 mg/mL (271.44 mM; ultrasonic and adjust pH to 9 with HCl)
CAS 數(shù)據(jù)庫459-86-9

安全數(shù)據(jù)

應(yīng)用領(lǐng)域

用途1
該品為治療成人急性粒細(xì)胞白血病和惡性淋巴瘤的藥物。

制備方法

方法1
由氨基胍碳酸鹽(見02050)縮合而得。將氨基脲碳酸鹽溶于無水乙醇,在室溫下滴加鹽酸,回流反應(yīng)1h后冷卻至30℃,繼續(xù)滴加鹽酸。冷卻至0℃,滴加丙酮醛。加畢,反應(yīng)6h。放置冷卻,過濾,濾餅經(jīng)洗滌、干燥、精制而得丙脒腙。收率約65%。

上下游產(chǎn)品信息

常見問題列表

制備
米托胍腙的合成方法:在配有回流冷凝器、溫度計(jì)、滴液漏斗、磁力攪拌器的500ml四口燒瓶中加入氨基胍碳酸鹽、甲醇(可或回收),開機(jī)攪拌,在22~28℃用2小時(shí)滴加濃鹽酸使PH=1,鹽酸滴加完畢在22~30℃繼續(xù)攪拌30分鐘,緩慢升溫到60±2℃并維持30分鐘后,降溫到22~28℃,用3小時(shí)滴加丙酮醛縮二甲醇,滴加丙酮醛縮二甲醇的過程中保持溫度在22~28℃,丙酮醛縮二甲醇滴加完畢繼續(xù)攪拌過夜,次日反應(yīng)液冷至5~10℃,過濾,用甲醇洗滌3次,每次10ml。濾液經(jīng)常壓回收重復(fù)使用;濾餅浸泡于100ml甲醇中,經(jīng)洗滌過濾、真空干燥,得米托胍腙,純度高達(dá)(HPLC)99.5%以上。
生物活性
Mitoguazone (Methylglyoxal-bis(guanylhydrazone)) 是一種具有有效抗腫瘤活性的合成多羰基衍生物。Mitoguazone 是一種可透過血腦屏障的競(jìng)爭(zhēng)性的 S-腺苷-蛋氨酸脫羧酶 (S-adenosyl-methionine decarboxylase) 抑制劑,可破壞多胺的生物合成。Mitoguazone 誘導(dǎo)細(xì)胞凋亡 (apoptosis),可抑制 HIV DNA 整合到單核細(xì)胞和巨噬細(xì)胞中的細(xì)胞 DNA 中。Mitoguazone 具可用于急性白血病,霍奇金淋巴瘤和非霍奇金淋巴瘤的研究。
體外研究

Mitoguazone competitively inhibits spermidine synthesis in lymphocytes at concentrations as low as 0.5 μg/mL. Levels of 30 μg/mL or more inhibit protein synthesis and mitochondrial respiration.
The ability of Mitoguazone to induce apoptosis by inhibiting the polyamine pathway is assessed in three Burkitt's lymphoma cell lines (Raji, Ramos and Daudi) and one prostate carcinoma cell line (MPC 3). Mitoguazone induces apoptosis in all the different human cancer cell lines tested in a concentration- and time-dependent way, and triggers a p53-independent programmed cell death in the human breast cancer MCF7 cell line.

體內(nèi)研究

The influence of different stages of leukemia P388 on the pharmacokinetics of the antineoplastic agent Mitoguazone in mice is investigated. Independent of the tumor stage investigated, the total clearance of mitoguazone is slightly reduced reflecting a moderate increase of AUC in the serum of leukemia-bearing animals. Furthermore, in an advanced tumor stage the drug levels in kidneys, liver, spleen and serum are found to be elevated to some extent in comparison to tumor-free controls in contrast to an earlier stage of leukemia.

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