In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
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 .
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 .
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.
 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.
|Physical Appearance||A solid|
|Storage||Store at -20°C|
|Solubility||≥38 mg/mL in DMSO with gentle warming, ≥22.55 mg/mL in EtOH with gentle warming, insoluble in H2O|
|Canonical SMILES||O=C1C2=CC(F)=CC(N[[email protected]@H](C3=CC=C(F)C=C3)[[email protected]@H]4C5=NC=NN5C)=C2C4=NN1|
|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 is a novel PARP inhibitor with IC50 of 0.58 nM(PARP1). It does not inhibit PARG and is highly sensitive to PTEN mutation.|
Quality Control & MSDS
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