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BMN-673 8R,9S

Cat. No. M4854

BMN-673 8R,9S Structure
Size Price Availability Quantity
2mg USD 100 In stock
5mg USD 150 In stock
10mg USD 255 In stock
50mg USD 650 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 380.35
Formula C19H14F2N6O
CAS Number 1207456-00-5
Purity >99%
Solubility DMSO
Storage at -20°C
References

Structure and preclinical characterization of BMN 673, a potent and orally active PARP inhibitor as an anticancer agent.
Yuqiao, et al. Mol Cancer Ther. 2011 Nov;10(11 Suppl).

Correlation of pharmacokinetics (PK), pharmacodynamics (PD) and in vivo antitumor activity of BMN 673 in preclinical models.
Ying, et al. Mol Cancer Ther. 2011 Nov;10(11 Suppl).

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BMN673 isomer

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: BMN-673 8R,9S supplier, PARP, inhibitors

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