- Cesium chloride
- DAPK Substrate Peptide
- GRI 977143
- Mdivi 1
- NQDI 1
| MelphalanDNA alkylating agent |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
Nature.2018 Nov;563(7731):407-411.Nature.2018 Jun 13.Nature.2018 Jun 27.Nature.2018 Mar 29;555(7698):673-677.Nature.2017 Sep 7;549(7670):96-100.Nature.2016 Apr 21;532(7599):398-401.
Science.2016 Aug 5;353(6299)594-8Nat Nanotechnol.2017 Dec;12(12):1190-1198.Nature Biotechnology.2017 Jun;35(6):569-576Nat Med.2018 Sep 17.Cell.2018 Dec 21. pii: S0092-8674(18)31561-7.Cell.Available online 25 October 2018.Cell.2018 Sep 27. pii: S0092-8674(18)31183-8.Cell.2018 Jun 28;174(1):172-186.e21.Cell.2018 Feb 22;172(5):1007-1021.e17.Cell.2017 Nov 30;171(6):1284-1300.e21.Cell.2017 Aug 17. pii: S0092-8674(17)30869-3.Cell.2017 Jul 13;170(2):312-323Nat Med.2018 Jan 29.Nat Med.2017 Nov;23(11):1342-1351.Cell.2017 Apr 6;169(2):286-300.Cell.2015 Aug 27;162(5):987-1002.Cell.2015 Feb 12;160(4):729-44.Nature Medicine.2017 Apr;23(4):493-500.Cancer Cell.2018 May 14;33(5):905-921.e5.Cancer Cell.2018 Apr 9;33(4):752-769.e8.Cancer Cell.2018 Mar 12;33(3):401-416.e8.Cancer Cell.2017 Aug 14;32(2):253-267.e5.Nat Methods.2018 Jul;15(7):523-526.Cell Stem Cell.2018 May 3;22(5):769-778.e4.Cell Stem Cell.2017 Nov 20. pii: S1934-5909(17)30375-2.Quality Control & MSDS
- View current batch:
- Purity = 98.00%
- COA (Certificate Of Analysis)
- MS (Mass Spectrometry)(Retest)
- NMR (Nuclear Magnetic Resonance)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
| Cell experiment [1]: | |
Cell lines | Human myeloma cell line RPMI 8226, neuroblastoma cell lines; SH-SY5Y, SK-N-AS, and SK-N-BE |
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. |
Reacting condition | 30-min |
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]: | |
Animal models | Immunodeficient mice bearing human ovarian tumors from A2780 cells |
Dosage form | Intraperitoneal injection, 11.7 mg/kg |
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. |
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. |
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 | Download SDF |
| Synonyms | N/A | ||
| Chemical Name | (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 | ||
| Formula | C13H18Cl2N2O2 | M.Wt | 305.2 |
| Solubility | ≥6.85mg/mL in DMSO | Storage | Store at RT |
| Physical Appearance | A solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
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.
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**捷向您推荐美国Trevigen的一款通用PARP分析试剂盒检测试剂盒。该试剂盒是检测凋亡前与凋亡中细胞提取液中PARP活性的理想方案，操作简单，重复性高。其通过检测96孔板上生物素标记的多聚ADP核糖聚合到邻近组蛋白的反应，从而确定已知的或可能的PARP抑制剂。试剂盒中的依托泊苷（Etoposide）是拓扑异构酶Ⅱ抑制剂，在拓扑异构酶Ⅱ切割完DNA后能够稳定该酶。在试剂盒中，依托泊苷作为凋亡诱导的对照参与检测。
通量PARP/凋亡分析试剂盒可广泛应用于1）检测原代、肿瘤等细胞的PARP活性；2）检测凋亡前后的PARP活性；3）利用细胞裂解液筛选PARP抑制剂。
试剂盒特色比色法/化学发光法，无放射性输出。96well，高通量检测。极大地节省了分析时间，提高了使用效率。高敏感性。能够检测到500个细胞中低至0.1mU的PARP。检测范围广。0.1-10mU。样本用量少。仅仅需要10-100ng的提取物。检测时间短。仅需要3h即可完成检测。
**捷向您提供一站式的PARP相关实验解决方案，除了高通量PARP/凋亡分析试剂盒，还有PARP体内药理动力学二代分析试剂盒(PDAII)和通用PAPR分析试剂盒外(含组蛋白包被可拆卸板)，以及相关抗体和重组蛋白。
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A.优点：
多重分析——一次分析可以检测16种干细胞相关的TF
定量比较——二个样本的差异可以定量分析和比较
步骤简单——探针温育、柱分离、板杂交和HRP检测
无需贵重仪器——无需如Luminex那样的贵重仪器
B.原理：
干细胞转录因子活性多重检测阵列试剂用于同时检测多种TF活性。该技术中，基于TFDNA结合位点的一致性序列，制备一系列生物素标记的探针。当探针混合物与核提取物一起温育时，每个探针寻找相应的TF，形成TF/探针复合物，通过柱离心纯化可以很容易与游离探针分开。结合的探针从混合物中分离出来，通过板杂交分析。板孔中预包被上与探针互补的特异序列，捕获的DNA探针进一步用链酶亲和素-HRP检测，化学发光检测仪测定发光强度（RLUs）。
