Detail of "16506-27-7"

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Cytotoxic efficacy of bendamustine in human leukemia and breast cancer cell lines

Cytotoxic efficacy of bendamustine in human leukemia and breast cancer cell lines. Konstantinov, S. M.; Kostovski, A.; Topashka-Ancheva, M.; Genova, M.; Berger, M. R. (Dept. of Pharmacology and Toxicology, Lab. for Experimental Chemotherapy, Faculty of Pharmacy at the Medical University of Sofia, Sofia 1000, Bulg.). Journal of Cancer Research and Clinical Oncology, 128(5), 271-278 (English) 2002 Springer-Verlag. CODEN: JCROD7. ISSN: 0171-5216. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) The purpose of this study was to characterize bendamustine's cytotoxic and apoptotic activity in a panel of leukemia and breast cancer cell lines in comparison to its clastogenicity in murine bone marrow. The cytotoxic effect of bendamustine was measured by the 3-(4,5-dimethylthiazol-2-yl)-2,5 diphenyltetrazolium bromide (MTT)-dye redn. assay. Induction of apoptosis was evidenced by DNA gel electrophoresis, nuclear staining, Western blot poly-(ADP-ribose) polymerase (PARP) cleavage, and flow cytometry. As a measure of hematol. toxicity, the formation of chromosomal aberrations was investigated in bone marrow cells isolated from mice treated with low non-toxic doses of bendamustine and lomustine. Bendamustine was preferably active against leukemic cells of lymphoid origin and was found to induce apoptosis in SKW-3 and BV-173 cells as shown by oligonucleosomal DNA and nuclear fragmentation, PARP cleavage, and formation of a sub-G1 fraction. There are some commonly used reagents like 16506-27-7 in this article. Myeloid and breast carcinoma cell lines were resistant towards bendamustine with the exception of HL-60 cells which exhibit an intermediate sensitivity. Bendamustine was found to have a very low clastogenic effect as compared with equimolar doses of lomustine. Taken together, the mode of action of bendamustine includes induction of apoptosis. The specific spectrum of activity and the unexpectedly low clastogenicity support the hypothesis that bendamustine in not a typical alkylating agent but exerts an addnl. mode of action, possibly as a purine antimetabolite. .

Antitumor sustained-release injection containing estrogen receptor antagonist and its synergistic agent from taxanes, alkylating agents and/or plant alkaloids

All Rights Reserved. Antitumor sustained-release injection containing estrogen receptor antagonist and its synergistic agent from taxanes, alkylating agents and/or plant alkaloids. Sun, Juan (Jinan Kangquan Pharmaceutical Science and Technology Co., Ltd., Peop. Rep. China). Faming Zhuanli Shenqing Gongkai Shuomingshu CN 1857217 A 8 Nov 2006, 28pp. (Chinese). (People's Republic of China). CODEN: CNXXEV. APPLICATION: CN 2010-200280 28 Mar 2006. DOCUMENT TYPE: Patent CA Section: 63 (Pharmaceuticals) The sustained-release injection is comprised of (A) sustained-release microsphere comprising antitumor effective constituent 0.5-60, sustained-release adjuvant 41-99.9 wt% and suspending agent 0.0-30.0 wt%; and (B) solvent. The antitumor effective constituent is selected from estrogen receptor antagonist and/or its synergistic agent which is selected from taxanes, alkylating agents and/or plant alkaloids. The estrogen receptor antagonist is selected from fulvestrant, anastrozole, exemestane, tamoxifen, or the mixt. thereof. The taxanes is selected from taxol, docetaxel, 2'-hydroxy-taxol, 10-deacetylbaccatin III, and 7-epi-taxol. The alkylating agent is selected from one of ambamustine, nimustine, bendamustine, lomustine, tallimustine, melphalan, etc., or the mixt. thereof. The plant alkaloid is selected from one of vincristine, vinblastine, vinleurosine, monocrotaline, etc., or the combination thereof. The sustained-release adjuvant is selected from one of a) polylactic acid; b) Polyglycolic acid-hydroxy acetic acid copolymer; c) polifeprosan; d) ethene-vinyl acetate copolymer; e) difatty acid-sebacic acid copolymer; f) poly(erucic acid dimer-sebacic acid) copolymer; g) poly(fumaric acid-sebacic acid) copolymer; h) xylitol, oligosaccharide, chondroitin, chitin, hyaluronic acid, collagens, etc.; or the mixt. thereof. The suspending agent is one of a) 0.5-3.0 % (sodium) CM-cellulose; b) 5-15 % mannitol; c) 5-15 % sorbitol; d) 0.1-1.5 % surfactant; e) 0.1-0.5 % tween 20; f) (iodine) glycerin, dimethicone, propylene glycol, or carbomer; g) 0.5-5 % sodium CM-cellulose + 0.1-0.In this experiment, several chemicals are used like 16506-27-7 and 107868-30-4 5 % tween 80; h) 5-20 % mannitol + 0.1-0.5 % tween 80; or i) 0.5-5 % sodium CM-cellulose + 5-20 % sorbitol + 0.1-0.5 % tween 80. .