Melphalan
(Synonyms: Alanine Nitrogen Mustard, Alkeran, NSC 8806, NSC 241286, L-Phenylalanine Mustard) 目录号 : GC12393
DNA alkylating agent
Cas No.:148-82-3
Sample solution is provided at 25 µL, 10mM.
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Melphalan is a DNA alkylating agent and inhibits DNA and RNA synthesis [1].
DNA alkylating agent attaches the alkyl group to the guanine base of DNA and inhibits DNA and RNA synthesis, which is necessary for cells to survive.
In PC-3 cells, melphalan inhibited cells growth with IC50 values of 0.074 μg/ml and 0.77 μg/ml for sequential dosing and single dosing, respectively, which suggested the sequential dosing was more effective [1].
In 12 patients with androgen-independent prostate cancer, melphalan provided some clinical benefits with manageable toxicity and the median survival was 23 weeks [1]. In 381 myeloma patients who received melphalan-based autologous stem cell transplant (Mel-ASCT), melphalan (200 mg/m2 body surface area (BSA)) led to oral mucositis (OM) in 75% of patients. And OM was severe in 21% patients. Patients with renal dysfunction have the greatest risk for severe OM when received a high mg/kg melphalan dose [2].
References:
[1]. Mougenot P, Bressolle F, Culine S, et al. In vitro cytotoxic effect of melphalan and pilot phase II study in hormone-refractory prostate cancer. Anticancer Res, 2006, 26(3B): 2197-2203.
[2]. Grazziutti ML, Dong L, Miceli MH, et al. Oral mucositis in myeloma patients undergoing melphalan-based autologous stem cell transplantation: incidence, risk factors and a severity predictive model. Bone Marrow Transplant, 2006, 38(7): 501-506.
| Cell experiment [1]: | |
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Cell lines |
Human myeloma cell line RPMI 8226, neuroblastoma cell lines; SH-SY5Y, SK-N-AS, and SK-N-BE |
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Preparation method |
The solubility of this compound in DMSO is >6.9 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
30-min |
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Applications |
Melphalan (5 and 10 pmol/l) resulted in an out-growth delay during the first 48 post-treatment. Melphalan treatment disclosed a relative increase of cells in S- and G-phases at 24 h followed by an accumulation of cells in G,-phase at 48 h. Treatment with high melphalan concentrations (20 and 40 pmol/l) the accumulation in the G-phase was more persistent. Melphalan treatment (20 pmol/l) dramatically decreased late S- and G,-phases. Exposure of a myeloma cell line (RPMI 8226) to a 30-minute pulse of melphalan (1-phenylalanine-mustard) resulted in a cell cycle progression delay characteristic for DNA cross-linking agents. Melphalan bound to DNA, RNA, and protein in cells in vitro. Melphalan induced chromosomal aberrations, sister chromatid exchange, micronuclei, mutations at the HPRT gene, and DNA damage in human cells in vitro. Melphalan induced transformation of C3H 10T1/2 and other cells. In cultured rodent cells, it induced chromosomal aberrations, sister chromatid exchange, gene mutations, and DNA damage. Melphalan induced aneuploidy and sex-linked recessive lethal mutations in Drosophila, and mutation in bacteria. |
| Animal experiment [3]: | |
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Animal models |
Immunodeficient mice bearing human ovarian tumors from A2780 cells |
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Dosage form |
Intraperitoneal injection, 11.7 mg/kg |
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Application |
In immunodeficient mice bearing human ovarian tumors from A2780 cells, melphalan (11.7 mg/kg, i.p.) severely inhibited the growth of previously untreated tumors, whereas the growth of tumors which had received prior treatment with melphalan was unaffected by the subsequent high dose. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. Fernberg J O, Lewensohn R, Skog S. Cell cycle arrest and DNA damage after melphalan treatment of the human myeloma cell line RPMI 8226[J]. European journal of haematology, 1991, 47(3): 161-167. [2]. MELPHALAN. Pharmaceuticals.Bookshelf [3]. Caffrey P B, Zhang Y, Frenkel G D. Rapid development of drug resistance in human ovarian tumor xenografts after a single treatment with melphalan in Vivo[J]. Anticancer research, 1998, 18(4C): 3021-3025. |
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| Cas No. | 148-82-3 | SDF | |
| 别名 | Alanine Nitrogen Mustard, Alkeran, NSC 8806, NSC 241286, L-Phenylalanine Mustard | ||
| 化学名 | (2S)-2-amino-3-[4-[bis(2-chloroethyl)amino]phenyl]propanoic acid | ||
| Canonical SMILES | C1=CC(=CC=C1CC(C(=O)O)N)N(CCCl)CCCl | ||
| 分子式 | C13H18Cl2N2O2 | 分子量 | 305.2 |
| 溶解度 | ≥ 6.85mg/mL in DMSO, <2.62 mg/mL in EtOH, <2.24 mg/mL in Water | 储存条件 | 4°C, protect from light |
| 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 | 3.2765 mL | 16.3827 mL | 32.7654 mL |
| 5 mM | 0.6553 mL | 3.2765 mL | 6.5531 mL |
| 10 mM | 0.3277 mL | 1.6383 mL | 3.2765 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。
Quality Control & SDS
- View current batch:
- Purity: >90.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet