Oxaliplatin

(rel)-Oxaliplatin is a DNA synthesis inhibitor. (rel)-Oxaliplatin causes DNA crosslinking damage, prevents DNA replication and transcription and induces apoptosis. (rel)-Oxaliplatin can be used for cancer research[1][2][3].

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

Signaling Pathways >> Cell Cycle/DNA Damage >> DNA/RNA Synthesis

(rel)-Oxaliplatin (24-72 hours; 2-128 μM; HCC, HCCLM3 and Hep3B cells) inhibits cell growth and induces apoptosis[1]. (rel)-Oxaliplatin (10 μM; 15-240 mins; CEM cells ) induces primary and secondary DNA lesions, including DNA cross-links (ISC) and DNA-protein cross-links (DPC)[2]. (rel)-Oxaliplatin (0.01 to 100 μM; 24 hours) potently inhibits bladder carcinoma cell lines RT4 and TCCSUP, ovarian carcinoma cell line A2780, colon carcinoma cell line HT-29, glioblastoma cell lines U-373MG and U-87MG, and melanoma cell lines SK-MEL-2 and HT-144 with IC50 of 11 μM, 15 μM, 0.17 μM, 0.97 μM, 2.95 μM, 17.6 μM, 30.9 μM and 7.85 μM, respectively[3] Cell Viability Assay[1] Cell Line: HCC, HCCLM3 and Hep3B cells Concentration: 24, 48 and 72 hours Incubation Time: 2, 4, 8, 16, 32, 64 and 128 μM Result: Decreased cell viability in a dose- and time-dependent manner. Western Blot Analysis[1] Cell Line: HCCLM3 and Hep3B cells Concentration: 48 hours Incubation Time: 10 μM Result: Down-regulated the expression of Bcl-2 and Bcl-xL, and increased the expression of Bax. Cell Cycle Analysis[1] Cell Line: HCCLM3 and Hep3B cells Concentration: 24 hours Incubation Time: 10 μM Result: Increased the percentage of apoptotic cells (17.70% for HCCLM3 cells; 21.19% for Hep3B cells).

(rel)-Oxaliplatin (5-10 mg/kg; i.p.; for 32 days; nude mice) inhibits tumor growth[1]. Animal Model: Nude mice[1] Dosage: 5 and 10 mg/kg Administration: Intraperitoneal injection; for 32 days Result: Reduced tumor volume in HCCLM3 tumor xenografts.

[1]. Woynarowski JM, et, al. Oxaliplatin-induced damage of cellular DNA. Mol Pharmacol. 2000 Nov;58(5):920-7.

[2]. Wang Z, et, al. Oxaliplatin induces apoptosis in hepatocellular carcinoma cells and inhibits tumor growth. Expert Opin Investig Drugs. 2009 Nov;18(11):1595-604.

[3]. Pendyala L, et, al. In vitro cytotoxicity, protein binding, red blood cell partitioning, and biotransformation of oxaliplatin. Cancer Res. 1993 Dec 15;53(24):5970-6.

MOLECULAR FORMULA :

C8-H14-N2-O4-Pt

MOLECULAR WEIGHT :

397.33

WISWESSER LINE NOTATION :

L6TJ AZ BZ &QVVQ &-PT-

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Intraperitoneal

SPECIES OBSERVED :

Rodent - mouse

DOSE/DURATION :

19800 ug/kg

TOXIC EFFECTS :

Details of toxic effects not reported other than lethal dose value

REFERENCE :

RIYADS Rinsho Yakuri. Clinical Pharmacology. (Nippon Rinsho Yakuri Gakkai, c/o Tokyo Ika Shika Daigaku Nanchi Shikkan Kenkyusho, 2-3-10 Suragadai, Kanda, Chiyoda-ku, Tokyo 101, Japan) V.1- 1970- Volume(issue)/page/year: 16,147,1985

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Intravenous

SPECIES OBSERVED :

Rodent - mouse

DOSE/DURATION :

30 mg/kg

TOXIC EFFECTS :

Details of toxic effects not reported other than lethal dose value

REFERENCE :

CTRRDO Cancer Treatment Reports. (Washington, DC) V.60-71, 1976-87. For publisher information, see JNCIEQ. Volume(issue)/page/year: 61,1519,1977