產(chǎn)品名稱：Iniparib 產(chǎn)品貨號(hào)：LC I-5432 產(chǎn)品規(guī)格：1 G Iniparib, also known as BSI-201, is a potent inhibitor of poly (ADP-ribose) polymerase-1 (PARP1). PARP1 plays an important role in the repair of DNA damage in cells that occurs naturally or that is induced by DNA-damaging chemotherapy. Iniparib had significant antitumor activity in vitro and in vivo, either alone or in combination with chemotherapy in preclinical studies. A randomized phase II clinical trial demonstrated that iniparib in combination with gemcitabine and carboplatin improved overall survival and clinical response in patients with metastatic triple-negative breast cancer (TNBC) when compared with gemcitabine and carboplatin alone. Liang, H. and Tan, A.R. "Iniparib, a PARP1 inhibitor for the potential treatment of cancer, including triple-negative breast cancer." IDrugs 13: 646-656 (2010). Iniparib was reduced transiently to 4-iodo-3-nitrosobenzamide by tumor cells at a very low rate, which inhibited PARP by zinc ejection and killed tumor cells. Mendeleyev, J., et al. "Potential chemotherapeutic activity of 4-iodo-3-nitrobenzamide. Metabolic reduction to the 3-nitroso derivative and induction of cell death in tumor cells in culture." Biochem. Pharmacol. 50: 705-714 (1995). Growth inhibition of E-ras 20 tumorigenic malignant cells by iniparib was improved 4-fold when cellular GSH content was diminished by buthionine sulfoximine (BSO), but the growth rate of CV-1 non-tumorigenic cells was not affected by the drug combination. Bauer, P.I., et al. "Anti-cancer action of 4-iodo-3-nitrobenzamide in combination with buthionine sulfoximine: inactivation of poly(ADP-ribose) polymerase and tumor glycolysis and the appearance of a poly(ADP-ribose) polymerase protease." Biochem. Pharmacol. 63: 455-462 (2002). Another CAS number previously assigned to iniparib, namely 937799-96-7 has been deleted by CAS and is no longer in use. Sold for laboratory or manufacturing purposes only; not for human, veterinary, food, or household use. This product is offered for R&D use in accordance with (i) 35 USC 271(e)+A13(1) in the U.S.; (ii) Section 69.1 of Japanese Patent Law in Japan; (iii) Section 11, No. 2 of the German Patent Act of 1981 in Germany; (iv) Section 60, Paragraph 5b of the U.K. Patents Act of 1977 in the U.K.; (v) Sections 55.2(1) and 55.2(6) and other common law exemptions of Canadian patent law; (vi) Section 68B of the Patents Act of 1953 in New Zealand together with the amendment of same by the Statutes Amendment Bill of 2002; (vii) such related legislation and/or case law as may be or become applicable in the aforementioned countries; and (viii) such similar laws and rules as may apply in various other countries. WARNING: Somewhat light-sensitive; avoid prolonged exposure to ambient light. Storage: Store at or below -20 ºC. Solubility: Soluble in DMSO at 200 mg/mL; soluble in ethanol at 12 mg/mL with warming; very poorly soluble in water; maximum solubility in plain water is estimated to be about 10-20 µM; buffers, serum, or other additives may increase or decrease the aqueous solubility. Disposal: A
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