Atrimustine

Atrimustine is a conjugate of chlorambucil and β-estradiol benzoate with the antitumor activity.

Product information

CAS Number: 75219-46-4

Molecular Weight: 720.72

Formula: C41H47Cl2NO6

Synonym:

Bestrabucil

KM2210

Chemical Name: (1S,3aS,3bR,9bS,11aS)-1-({2-[(4-{4-[bis(2-chloroethyl)amino]phenyl}butanoyl)oxy]acetyl}oxy)-3a,3b,9b-trihydrogenio-11a-methyl-1H,2H,3H,3aH,3bH,4H,5H,9bH,10H,11H,11aH-cyclopenta[a]phenanthren-7-yl benzoate

Smiles: C[C@]12CC[C@H]3[C@@H](CCC4=CC(=CC=C43)OC(=O)C3C=CC=CC=3)[C@@H]1CC[C@@H]2OC(=O)COC(=O)CCCC1C=CC(=CC=1)N(CCCl)CCCl

InChiKey: IFJUINDAXYAPTO-UUBSBJJBSA-N

InChi: InChI=1S/C41H47Cl2NO6/c1-41-21-20-34-33-17-15-32(49-40(47)29-7-3-2-4-8-29)26-30(33)12-16-35(34)36(41)18-19-37(41)50-39(46)27-48-38(45)9-5-6-28-10-13-31(14-11-28)44(24-22-42)25-23-43/h2-4,7-8,10-11,13-15,17,26,34-37H,5-6,9,12,16,18-25,27H2,1H3/t34-,35-,36+,37+,41+/m1/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

Atrimustine (Bestrabucil), a conjugate of chlorambucil and β-estradiol benzoate, has high affinity for tumor cells and enhances the antitumor activity of chlorambucil.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.

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.
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.

Products are for research use only. Not for human use.