Atrimustine (Bestrabucil)
(Synonyms: 阿莫司汀; Bestrabucil; KM2210) 目录号 : GC34155Atrimustine (Bestrabucil) 是苯丁酸氮芥和 β-estradiol benzoate 的结合物,具有抗肿瘤活性。
Cas No.:75219-46-4
Sample solution is provided at 25 µL, 10mM.
Atrimustine is a conjugate of chlorambucil and β-estradiol benzoate with the antitumor activity.
Atrimustine (Bestrabucil), a conjugate of chlorambucil and β-estradiol benzoate, has high affinity for tumor cells and enhancesthe antitumor activity of chlorambucil[1].The effect of Atrimustine (Bestrabucil), a benzoate of an estradiol-chlorambucil conjugate, is examined on the production of growth factor(s) by Shionogi carcinoma 115 (SC-115) cells, an androgen-responsive cultured cancer cell line. At Atrimustine concentrations of 100 nM-10 μM, concentration-dependent inhibition of growth factor production by SC-115 cells can be demonstrated by 3H-thymidine uptake assay[2].
[1]. Ezaki K, et al. A combination trial of human lymphoblastoid interferon and bestrabucil (KM2210) for adult T-cell leukemia-lymphoma. Cancer. 1991 Aug 15;68(4):695-8. [2]. Akaza H, et al. Inhibitory effects of bestrabucil, a conjugate of chlorambucil and estradiol, on the production of androgen-induced growth factor(s) by Shionogi carcinoma 115 cells. Int J Urol. 1994 Mar;1(1):67-73.
Cell experiment: | In the culture system containing 10 nM Testosterone, Atrimustine (Bestrabucil) exhibits a statistically significant inhibition of SC-115 cell growth at concentrations of 10 μM and 1 μM. Mixtures of Estradiol and Chlorambucil also significantly inhibit the growth of SC- 115 cells at concentrations of 1 μM and 100 nM. The inhibitory effect at day 7 of culture is regarded as similar for 10 μM Atrimustine and 1 μM of the mixture. At 10 μM, Atrimustine inhibits the growth of SC-115 cells to the sarve degree as the control culture without Testosterone and this concentration of Atrimustine is taken as the IC50. Thus, in experiment 2, 10 μM Atrimustine is used in the CM of SC-115 cells to study the inhibition of growth by Atrimustine [2]. |
References: [1]. Ezaki K, et al. A combination trial of human lymphoblastoid interferon and bestrabucil (KM2210) for adult T-cell leukemia-lymphoma. Cancer. 1991 Aug 15;68(4):695-8. |
Cas No. | 75219-46-4 | SDF | |
别名 | 阿莫司汀; Bestrabucil; KM2210 | ||
Canonical SMILES | C[C@@]1([C@H]2OC(COC(CCCC3=CC=C(N(CCCl)CCCl)C=C3)=O)=O)[C@](CC2)([H])[C@@](CCC4=CC(OC(C5=CC=CC=C5)=O)=CC=C64)([H])[C@]6([H])CC1 | ||
分子式 | C41H47Cl2NO6 | 分子量 | 720.72 |
溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
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1 mg | 5 mg | 10 mg | |
1 mM | 1.3875 mL | 6.9375 mL | 13.875 mL |
5 mM | 0.2775 mL | 1.3875 mL | 2.775 mL |
10 mM | 0.1388 mL | 0.6938 mL | 1.3875 mL |
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% DMSO % % Tween 80 % saline | ||||||||||
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2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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