Iniparib **

产品名称：Iniparib
产品货号：LC  I-5432 
产品规格：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

产品留言

标题

联系人

联系电话

内容

验证码

点击换一张

注：1.可以使用快捷键Alt+S或Ctrl+Enter发送信息!
2.如有必要,请您留下您的详细联系方式!