| BMN-673 8R,9SInactive form of BMN 673, used as negative control |
Sample solution is provided at 25 µL, 10mM.
Quality Control & MSDS
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- Purity = 98.48%
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Chemical structure
Related Biological Data
Related Biological Data
Related Biological Data
| BMN-673 8R,9S is an inactive form of BMN 673 and can be used as negative control. | ||||||
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| Cas No. | 1207456-00-5 | SDF | Download SDF |
| Synonyms | (8R,9S)-BMN-673 | ||
| Chemical Name | (8R,9S)-5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-8,9-dihydro-2H-pyrido[4,3,2-de]phthalazin-3(7H)-one | ||
| Canonical SMILES | O=C1C2=CC(F)=CC(N[C@@H](C3=CC=C(F)C=C3)[C@@H]4C5=NC=NN5C)=C2C4=NN1 | ||
| Formula | C19H14F2N6O | M.Wt | 380.35 |
| Solubility | ≥38 mg/mL in DMSO with gentle warming, ≥22.55 mg/mL in EtOH with gentle warming, <2.11 mg/ml="" in="" h2o=""> | Storage | Store at -20°C |
| Physical Appearance | A solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
BMN-673 8R,9S is an inactive form of BMN 673 and can be used as negative control.
PARP1/2 inhibitors are a class of anticancer agents that target tumor-specific defects in DNA repair. BMN 673 is a highly potent PARP1/2 inhibitor.In vitro: BMN 673 is a potent PARP1/2 inhibitor, but it does not inhibit other enzymes that we have tested. BMN673 exhibits selective antitumor cytotoxicity and elicits DNA repair biomarkers at much lower concentrations than earlier generation PARP1/2 inhibitors. BMN 673 targeted tumor cells with BRCA1, BRCA2, or PTEN gene defects selectively with 20- to more than 200-fold greater potency than existing PARP1/2 inhibitors in vitro [1]. In vivo: BMN 673 is readily orally bioavailable, with more than 40% absolute oral bioavailability in rats when dosed in CMC. Orally BMN 673 elicited remarkable antitumor activity in mice; xenografted tumors that carry defects in DNA repair due to BRCA mutations or PTEN deficiency were profoundly sensitive to oral BMN 673 treatment at well-tolerated doses. Synergistic antitumor effects were also found when BMN 673 was combined with temozolomide, SN38, or platinum drugs [1]. Clinical trial: Pharmacokinetics (PK), pharmacodynamics (PD), safety and anti-tumor activity of BMN 673 were evaluated in a 2-stage dose-escalation study with 3-6 patients (pts)/dose level. Results showed BMN 673 was well tolerated with impressive anti-tumor activity in pts with BRCA mut with a single agent recommended Phase II trial dose of 1000 μg/d due to dose-limiting thrombocytopenia. Reference:[1] Shen Y, Rehman FL, Feng Y, Boshuizen J, Bajrami I, Elliott R, Wang B, Lord CJ, Post LE, Ashworth A. BMN 673, a novel and highly potent PARP1/2 inhibitor for the treatment of human cancers with DNA repair deficiency. Clin Cancer Res. 2013;19(18):5003-15.
