V-4703 Veliparib, Free Base, >99%

VLP-104 VLP-103 VLP-102 VLP-101

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• Veliparib, also known as ABT-888, is a potent inhibitor of PARP-1 and PARP-2, with Ki values of 5.2 nM and 2.9 nM, respectively. It was demonstrated to have good oral bioavailability, to cross the blood-brain barrier well, to have modest antitumor activity alone, and to potentiate temozolomide, platinums, cyclophosphamide, and radiation in syngeneic and xenograft tumor models. Donawho C.K., et al. "ABT-888, an orally active poly(ADP-ribose) polymerase inhibitor that potentiates DNA-damaging agents in preclinical tumor models." Clin. Cancer Res. 13: 2728-2737 (2007).
• This research compound is the free base form of veliparib. We also offer the dihydrochloride salt form; please see Veliparib, Dihydrochloride Salt, Cat. No. [V-4799]
• A phase 1 clinical study demonstrated that the combination of veliparib with metronomic cyclophosphamide was well tolerated and showed promising activity in a subset of patients with refractory solid tumors and lymphomas and with BRCA mutations. Kummar S., et al. "A phase I study of veliparib in combination with metronomic cyclophosphamide in adults with refractory solid tumors and lymphomas." Clin. Cancer Res. 18: 1726-1734 (2012).
• Pressure-induced myogenic tone was potentiated while endothelium-dependent relaxation was reduced in diabetic mice compared with control mice. PARP-1 inhibitors INO-1001 and veliparib significantly reduced the potentiation of myogenic tone, improved endothelium-dependent relaxation, restored endothelial NO synthase phosphorylation and cGMP, and reduced cleaved PARP-1. PARP-1 inhibitors may be used to overcome diabetic microvascular dysfunction. Choi S.K., et al. "Poly(ADP-ribose) polymerase 1 inhibition improves coronary arteriole function in type 2 diabetes mellitus." Hypertension 59: 1060-1068 (2012).
• This veliparib product is the free base form, whose CAS number is given above. The CAS number of the dihydrochloride salt form is 912445-05-7.
• 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.
• Not available in some countries; not available to some institutions; not available for some uses.