Talazoparib (BMN-673) 是一种高效的,具有口服活性的 PARP 1/2 抑制剂。Talazoparib 抑制 PARP1 和 PARP2 酶活性的 Ki 值分别为 1.2 nM 和 0.87 nM。Talazoparib 具有抗肿瘤活性。
Front Oncol. 2022 Aug 16;12:940377.
Effectiveness of PARP inhibition in enhancing the radiosensitivity of 3D spheroids of head and neck squamous cell carcinoma
BMN673 (Talazoparib) purchased from AbMole
BMC Biol. 2021 May 20;19(1):108.
Very long intergenic non-coding (vlinc) RNAs directly regulate multiple genes in cis and trans
BMN673 (Talazoparib) purchased from AbMole
Clin Cancer Res. 2020 Oct 15;26(20):5462-5476.
A Preclinical Trial and Molecularly Annotated Patient Cohort Identify Predictive Biomarkers in Homologous Recombination-deficient Pancreatic Cancer
BMN673 (Talazoparib) purchased from AbMole
Proc Natl Acad Sci U S A. 2019 Nov 5;116(45):22609-22618.
DNA methyltransferase inhibitors induce a BRCAness phenotype that sensitizes NSCLC to PARP inhibitor and ionizing radiation.
BMN673 (Talazoparib) purchased from AbMole
Nat Commun. 2019 Dec 20;10(1):5799.
Novel approach reveals genomic landscapes of single-strand DNA breaks with nucleotide resolution in human cells.
BMN673 (Talazoparib) purchased from AbMole
US Patent. 2019 Jul 30.
THERAPY REGIMEN AND METHODS TO SENSITIZE CANCER CELLS TREATED WITH EPIGENETIC THERAPY TO PARP INHIBITORS IN MULTIPLE CANCERS
BMN673 (Talazoparib) purchased from AbMole
Nat Commun. 2018 Nov 12;9(1):4760.
Defective DNA damage repair leads to frequent catastrophic genomic events in murine and human tumors.
BMN673 (Talazoparib) purchased from AbMole
Cancer Cell. 2016 Oct 10;30(4):637-650.
Enhancing the Cytotoxic Effects of PARP Inhibitors with DNA Demethylating Agents – A Potential Therapy for Cancer
BMN673 (Talazoparib) purchased from AbMole
Cancer Lett. 2015 Aug 1;364(1):8-16.
Increased in vitro and in vivo sensitivity of BRCA2-associated pancreatic cancer to the poly(ADP-ribose) polymerase-1/2 inhibitor BMN 673.
BMN673 (Talazoparib) purchased from AbMole
Cell Rep. 2014 Nov 6;9(3):829-41.
Targeting the DNA repair pathway in Ewing sarcoma.
BMN673 (Talazoparib) purchased from AbMole
Cell Experiment | |
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Cell lines | Capan-1 and MIA PaCa-2 |
Preparation method | Real-time cell analysis (xCELLigence) |
Concentrations | |
Incubation time | 48 h |
Animal Experiment | |
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Animal models | Patient-derived xenograft (PDX) model |
Formulation | Solubilized in DMSO and diluted with PBS containing 10% dimethylacetamide (Sigma-Aldrich) and 6% Solutol (Sigma-Aldrich). |
Dosages | 0.33 mg/kg, 0.05 cc, once daily |
Administration | oral gavage |
Molecular Weight | 380.35 |
Formula | C19H14F2N6O |
CAS Number | 1207456-01-6 |
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 |
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.
Related PARP Products |
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NMS-P515
NMS-P515 is a potent inhibitor of PARP-1 both in biochemical (Kd: 0.016 μM) and cellular (IC50: 0.027 μM) assays. |
OM-153
OM-153 is a potent, orally active tankyrase inhibitor with IC50 of 13 nM for tankyrase 1 and 2 nM for tankyrase 2 (TNKS1/2). OM-153 inhibited luciferase based Wnt/β-catenin signal transduction reporter activity with IC50 of 0.63 nM. OM-153 inhibits Wnt/β-catenin signal transduction and proliferation in COLO 320DM. |
Amelparib
Amelparib is a potent, water soluble PARP-1 inhibitor with oral activity. |
Veliparib dihydrochloride
Veliparib (dihydrochloride) is a potent inhibitor of PARP1 and PARP2 with Kis of 5.2 nM and 2.9 nM in cell-free assays, respectively. |
Talazoparib tosylate
Talazoparib tosylate (BMN 673ts) is a novel, potent and orally available PARP1/2 inhibitor with an IC50 of 0.57 nM for PARP1. |
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