Atrimustine(Synonyms: 阿莫司汀; Bestrabucil; KM2210)

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Atrimustine (Synonyms: 阿莫司汀; Bestrabucil; KM2210)

Atrimustine 是苯丁酸氮芥与 β-雌二醇苯甲酸酯的结合物,具有抗肿瘤活性。

Atrimustine(Synonyms: 阿莫司汀; Bestrabucil;  KM2210)

Atrimustine Chemical Structure

CAS No. : 75219-46-4

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生物活性

Atrimustine is a conjugate of chlorambucil and β-estradiol benzoate with the antitumor activity.

体外研究
(In Vitro)

Atrimustine (Bestrabucil), a conjugate of chlorambucil and β-estradiol benzoate, has high affinity for tumor cells and enhances the 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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

720.72

Formula

C41H47Cl2NO6

CAS 号

75219-46-4

中文名称

阿莫司汀

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [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 Assay
[2]

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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献
  • [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.

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