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BMN673 is an orally bioavailable inhibitor of the nuclear enzyme poly (ADP-ribose) polymerase (PARP) with potential antineoplastic activity. PARP inhibitor BMN-673 selectively binds to PARP and prevents PARP-mediated DNA repair of single strand DNA breaks via the base-excision repair pathway. BMN-673 has been proven to be highly active in mouse models of human cancer and also appears to be more selectively cytotoxic with a longer half-life and better bioavailability as compared to other compounds in development. BMN 673 selectively kills cancer cells with BRCA-1 or BRCA-2 mutations. Oral dosing of BMN 673 results in complete regression of the BRCA-deficient tumors in xenograft tumor model studies. In addition, we found that tumor cells with PTEN mutation are highly sensitive to BMN 673 treatment in vitro. Xenograft tumor models that harbor PTEN deficiency responded to oral BMN 673 treatment with significant tumor growth delay. Currently, BMN 673 is in phase 1 clinical trials with solid tumors or hematological malignancies.
| Molecular Weight | 380.35 |
| Formula | C19H14F2N6O |
| CAS Number | 1207456-00-5 |
| Solubility (25°C) | DMSO ≥ 30 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related PARP Products |
|---|
| ABT-888
ABT-888 (Veliparib) is a potent inhibitor of PARP-1 and PARP-2 with Ki values of 5.2nM and 2.9nM respectively. |
| AG-014699 phosphate
AG-014699 (PF-01367338, Rucaparib) is a PARP inhibitor with a Ki of 1.4 nM. |
| AG14361
AG14361 is a novel poly (ADP-ribose) polymerase-1 inhibitor with a GI50 of 10.9 µM. |
| AZD2281 (Olaparib)
AZD 2281 (Olaparib, KU-0059436) is a potent PARP (poly ADP-ribose polymerase) inhibitorwith IC50 of 5 and 1 nM for PARP-1and PARP-2 respectively. Olaparib is an autophagy and mitophagy activator. |
| Talazoparib
Talazoparib (BMN-673) is a highly potent, orally active PARP1/2 inhibitor.Talazoparib inhibits PARP1 and PARP2 enzyme activity with Kis of 1.2 nM and 0.87 nM, respectively. Talazoparib has antitumor activity. |
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