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 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.

720.72

C₄₁H₄₇Cl₂NO₆

75219-46-4

阿莫司汀

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

• [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.

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.

• [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.