Atrimustine (Bestrabucil)
(Synonyms: 阿莫司汀; Bestrabucil; KM2210) 目录号 : GC34155
Atrimustine (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.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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. | |
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.
| 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 |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
[Clinical trial of Bestrabucil (KM 2210) in hematopoietic malignancies]
Gan No Rinsho 1986 Sep;32(11):1443-50.PMID:2877106doi
Thirteen patients with hematological neoplasms were treated with Bestrabucil (100 mg/day po, total dose 700-9,900 mg), which is the benzoate of an estradiol-chlorambucil conjugate. The diseases from which they suffered consisted of T-cell leukemia (3), lymphoma (3), myeloma (5) and essential thrombocytosis (2). Although this drug was less effective against myeloma, the other diseases were more or less relieved with this medication. That is, Bestrabucil was effective in all three patients with T-cell leukemia, both with essential thrombocytosis and two of the three with lymphoma. It is most interesting that adult T-cell leukemia (ATL) cells decreased remarkably with Bestrabucil, along with the disappearance of several symptoms (bone pain, hypercalcemia etc.). The main side effects during this medication were mammary pain (eight of 13 patients, 62%), anorexia (five of 13 patients, 39%) and loss of libido (three of 13 patients, 23%), but neither severe myelosuppression nor hepatorenal dysfunction was induced.
[Bestrabacil: a possible target-oriented anticancer agent]
Gan To Kagaku Ryoho 1984 Oct;11(10):2115-24.PMID:6548354doi
Bestrabucil, the benzoate of an estradiol-chlorambucil conjugate, was initially developed as a target-oriented anticancer agent for breast cancers with positive estrogen receptors, by conjugating a tumoricidal agent, chlorambucil, to a vehicle, estradiol. Further studies, however, revealed that regardless of the presence of estrogen receptors, Bestrabucil selectively accumulates in malignant tumor cells. The unique feature of Bestrabucil, selective affinity to tumor cells, was demonstrated in in vitro and in vivo studies. Significantly larger amounts of 3H-bestrabucil accumulated in malignant cells (3T3-SV40 transformed) than in normal cells (3T3). In vitro inhibition effects of Bestrabucil on cell growth was observed only in malignant cells. Selective accumulation of Bestrabucil in malignant tumor tissues was also demonstrated in in vivo experiments. After a single oral administration of 100 mg/kg of Bestrabucil to female Wistar rats bearing Walker 256 carcinoma, Bestrabucil accumulated significantly occurred in tumor tissues with little or no accumulation in normal tissues and blood. Anti-tumor effects and toxicities of Bestrabucil and chlorambucil, were compared using Walker 256 carcinoma. Bestrabucil exerted its antitumor effects with little change in leucocyte counts in the peripheral blood, whereas chlorambucil showed significant side effects. Finally, selective accumulation of Bestrabucil in malignant tumor tissues, was demonstrated clinically. Tumor specimens obtained during the operation of patients with various types of cancer, 24 hours after oral administration of 100 mg of Bestrabucil, contained significantly larger amounts of Bestrabucil compared with adjacent normal tissues. Clinical trials of Bestrabucil are being carried out at present. Bestrabucil seems to be a promising target-oriented anticancer agent and deserves further investigation.
A combination trial of human lymphoblastoid interferon and Bestrabucil (KM2210) for adult T-cell leukemia-lymphoma
Cancer 1991 Aug 15;68(4):695-8.PMID:1855169DOI:10.1002/1097-0142(19910815)68:4<695::aid-cncr2820680405>3.0.co;2-k.
Both human lymphoblastoid interferon (HLBI) and Bestrabucil, the conjugate of chlorambucil and beta-estradiol, have antitumor activity against adult T-cell leukemia-lymphoma (ATLL). Because an in vitro study showed that these two agents combined had a synergistic antiproliferative effect on MOLT-4 and WI-38VA13 cell lines, the authors evaluated the clinical efficacy of this combination in a pilot study with a poor-risk group of ATLL patients. The patients were treated daily with 6 x 10(6) IU of HLBI subcutaneously and 100 mg of Bestrabucil orally. In patients with lymphoma-type ATLL or hypercalcemia, prednisolone also was given daily. Of 12 patients suitable for evaluation, nine had partial responses, one had a minor response, and two had no response. All five patients with skin infiltration and both patients with hypercalcemia responded. A history of prior chemotherapy did not affect the response rate. The time to clinical response was 3 to 16 days (median, 11 days) after initiation of treatment. The response duration was 4 to 108+ weeks (median, 9 weeks), but all patients except one relapsed, even during continuing treatment. No serious side effects were observed. Although the response rate with this combination treatment was high, the response duration was short, and other treatments would have to be added to achieve control of this aggressive disease.
[Bestrabucil-induced complete remission in a case of follicular lymphoma, medium-sized cell type, stage IV (leukemic)]
Gan No Rinsho 1986 Sep;32(11):1491-4.PMID:3534347doi
Bestrabucil, a chlorambucil-estradiol conjugate known to accumulate in malignant cells irrespective of the presence or absence of estrogen receptor, was administered to a 41-year-old man with follicular lymphoma, medium-sized cell type (LSG classification) stage IV (leukemic). A daily dose of 100 mg was given for two weeks and then 200 mg for a week. The WBC dropped from 43,100/mm3 with 82% abnormal lymphocytes to 12,800/mm3, and the drug was discontinued. It was resumed two weeks later at a daily dose of 50 mg. Four weeks thereafter, complete remission was obtained with the disappearance of all peripheral adenopathies and abnormal cells from the bone marrow. The patient remains disease-free for more than eight months on a maintenance dose of 50 mg per day. Transient erythema and gynecomastia have been the only side effects so far observed.
[Early phase II trial of Bestrabucil in hematological malignancies]
Gan To Kagaku Ryoho 1986 Jun;13(6):2216-22.PMID:3459398doi
Thirty-three patients with various hematological malignancies were treated with Bestrabucil, the benzoate of an estradiol-chlorambucil conjugate, at doses of 50-300 mg daily p.o., consecutively. Nineteen patients had previously received chemotherapy. Of 29 evaluable patients, there were one CR and three PRs among 6 patients with chronic lymphocytic leukemia, two CRs and one PR among 4 patients with malignant lymphoma, two PRs among 3 patients with adult T-cell leukemia, one PR among 4 patients with macroglobulinemia, one PR for one patient with essential thrombocythemia, and one PR for a patient with chronic myelocytic leukemia. Main side effects included G1 symptoms (14%), estradiol-related symptoms (24%) and myelosuppression (32%).