Melphalan

Catalog No.S8266 Batch:S826603

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Technical Data

Formula

C13H18Cl2N2O2

Molecular Weight 305.20 CAS No. 148-82-3
Solubility (25°C)* In vitro DMSO 3.5 mg/mL (11.46 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description Melphalan (Alkeran, Sarcolysin, L-PAM) is a phenylalanine derivative of nitrogen mustard with antineoplastic activity.This product is a hazardous chemical (acute toxicity/flammable/skin corrosive). Please use it while wearing a protective face mask, gloves, and clothing.
In vitro Exposure of a myeloma cell line (RPMI 8226) to a 30-minute pulse of melphalan (1-phenylalanine-mustard) results in a cell cycle progression delay characteristic for DNA cross-linking agents[1]. Melphalan has been shown to bind to DNA, RNA, and protein in cells in vitro. Melphalan induces chromosomal aberrations, sister chromatid exchange, micronuclei, mutations at the HPRT gene, and DNA damage in human cells in vitro. It also induces transformation of C3H 10T1/2 and other cells. In cultured rodent cells, it induces chromosomal aberrations, sister chromatid exchange, gene mutations, and DNA damage. In addition, it induces aneuploidy and sex-linked recessive lethal mutations in Drosophila, and mutation in bacteria[3].
In vivo Melphalan has been tested in mice by oral, intraperitoneal, and dermal application; in rats by intraperitoneal injection, and in monkeys by oral administration. In mice, the administration of melphalan produced forestomach papillomas, lymphosarcomas, and skin and lung tumours. In rats, melphalan caused mammary gland tumours, and peritoneal sarcomas. Results in monkeys were inconclusive[3].

Protocol (from reference)

Animal Study:[2]
  • Animal Models

    Tg.AC mice

  • Dosages

    0.25, 1, and 4 mg/kg weekly

  • Administration

    Topical administration/oral gavage

Customer Product Validation

Data from [Data independently produced by , , Blood, 2016, 127(9):1138-50. ]

Selleck's Melphalan has been cited by 18 publications

Therapeutic potential of anti-PIK3CG treatment for multiple myeloma via inhibiting c-Myc pathway [ Heliyon, 2024, 10(1):e23165] PubMed: 38163179
Identification and targeting of protein tyrosine kinase 7 (PTK7) as an immunotherapy candidate for neuroblastoma [ Cell Rep Med, 2023, 4(6):101091] PubMed: 37343516
Deneddylation of ribosomal proteins promotes synergy between MLN4924 and chemotherapy to elicit complete therapeutic responses [ Cell Rep, 2023, 42(8):112925] PubMed: 37552601
Proteomic profiling reveals CDK6 upregulation as a targetable resistance mechanism for lenalidomide in multiple myeloma [ Nat Commun, 2022, 13(1):1009] PubMed: 35197447
NEDD4L binds the proteasome and promotes autophagy and bortezomib sensitivity in multiple myeloma [ Cell Death Dis, 2022, 13(3):197] PubMed: 35236820
ISG20L2 suppresses bortezomib antimyeloma activity by attenuating bortezomib binding to PSMB5 [ JCI Insight, 2022, 7(19)e157081] PubMed: 36040812
Inhibition of the Protein Arginine Methyltransferase PRMT5 in High-Risk Multiple Myeloma as a Novel Treatment Approach [ Front Cell Dev Biol, 2022, 10:879057] PubMed: 35757005
HAPLN1 confers multiple myeloma cell resistance to several classes of therapeutic drugs [ PLoS One, 2022, 17(12:e0274704)] PubMed: 36480501
Comprehensive CRISPR-Cas9 screens identify genetic determinants of drug responsiveness in multiple myeloma [ Blood Adv, 2021, 5(9):2391-2402] PubMed: 33950175
Novel Peptide-drug Conjugate Melflufen Efficiently Eradicates Bortezomib-resistant Multiple Myeloma Cells Including Tumor-initiating Myeloma Progenitor Cells [ Hemasphere, 2021, 5(7):e602] PubMed: 34136753

RETURN POLICY
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.