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001028 Veliparib CAS: 912444-00-9

Specifications
References
CAS Number
912444-00-9
Grade
Purified
Molecular Formula
C13H16N4O
Molecular Weight
244.29
EU Commodity Code
38220090
Shipping Temp
RT
Storage Temp
RT
2-[(2R)-2-Methyl-2-pyrrolidinyl]-1H-benzimidazole-7-carboxamide; A 861695; ABT 888

ABT-888 is a potent, orally bioavailable PARP-1/-2 inhibitor shown to potentiate DNA damaging agents. The ability to potentiate temozolomide (TMZ) and develop a biological marker for PARP inhibition was evaluated in vivo.

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).
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.
Appearance
White to off-white crystalline solid.
Purity
≥99% (HPLC, TLC)
Melting Point
186-188°C
Solubility
DMSO, Methanol
Source
Synthetic
Purity
≥99% (HPLC, TLC)
Form
White to off-white crystalline solid.
Important Note
This product as supplied is intended for research use only, not for use in human, therapeutic or diagnostic applications without the expressed written authorization of United States Biological.
References
Virag, L., et al.: Pharmacol. Rev., 54, 375
USBio References
No references available
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