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Talazoparib tosylate
CAS No. 1373431-65-2
Talazoparib tosylate( —— )
Catalog No. M33505 CAS No. 1373431-65-2
Talazoparib tosylate is a novel and potent PARP1/2 (n IC50: 0.57 nM for PARP1).
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 1 mL x 10 mM in DMSO | 65 | In Stock |
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| 2MG | 33 | In Stock |
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| 5MG | 53 | In Stock |
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| 10MG | 77 | In Stock |
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| 25MG | 130 | In Stock |
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| 50MG | 184 | In Stock |
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| 100MG | 305 | In Stock |
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| 200MG | 423 | In Stock |
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| 500MG | Get Quote | In Stock |
|
| 1G | Get Quote | In Stock |
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Biological Information
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Product NameTalazoparib tosylate
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NoteResearch use only, not for human use.
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Brief DescriptionTalazoparib tosylate is a novel and potent PARP1/2 (n IC50: 0.57 nM for PARP1).
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DescriptionTalazoparib 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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In VitroTalazoparib is a potent PARP1/2 inhibitor (PARP1 IC50=0.57 nM), it has no effect on PARG activity at concentrations up to 1 μM. Talazoparib binds to PARP1 with a dissociation constant (KD) of 0.29 nM. Talazoparib inhibits PARP1 and -2 to a similar extent, with Kis of 1.20 and 0.85 nM, respectively. Talazoparib selectively targets tumor cells with BRCA1, BRCA2, or PTEN gene defects with 20- to more than 200-fold greater potency than existing PARP1/2 inhibitors. Talazoparib targets tumor cells with homologous recombination gene defects. Tumor models that are either BRCA1-deficient (MX-1 and SUM149) or BRCA2-deficient (Capan-1) are profoundly sensitive to Talazoparib. Talazoparib induces nuclear γ-H2AX foci at concentrations as low as 100 pM.
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In VivoTalazoparib is readily orally bioavailable, with more than 40% absolute oral bioavailability in rats when dosed in carboxylmethyl cellulose. Oral administration of Talazoparib elicits remarkable antitumor activity; xenografted tumors that carry defects in DNA repair due to BRCA mutations or PTEN deficiency are profoundly sensitive to oral Talazoparib treatment at well-tolerated doses in mice. Synergistic or additive antitumor effects are also found when Talazoparib is combined with temozolomide, SN38, or platinum drugs.
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Synonyms——
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PathwayCell Cycle/DNA Damage
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TargetPARP
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RecptorPARP
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Research Area——
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Indication——
Chemical Information
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CAS Number1373431-65-2
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Formula Weight552.55
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Molecular FormulaC26H22F2N6O4S
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Purity>98% (HPLC)
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SolubilityIn Vitro:?DMSO : ≥ 108 mg/mL (195.46 mM) H2O : < 0.1 mg/mL (insoluble)
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SMILESCc1ccc(cc1)S(O)(=O)=O.Cn1ncnc1[C@@H]1[C@H](Nc2cc(F)cc3c2c1n[nH]c3=O)c1ccc(F)cc1
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Chemical Name——
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
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OUL35
OUL35 is a selective PARP-10 inhibitor, and small-molecule ARTD10 inhibitor. OUL35 has been shown to rescue cells from ARTD10-induced cell death.
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Rucaparib Camsylate
Rucaparib Camsylate is a PARP inhibitor (PARP1,Ki of 1.4 nM). Rucaparib Camsylate also displays binding affinity to eight other PARP domains. Rucaparib is the most effective PARP inhibitor in enzyme assays (Ki: 1.4 nM). Rucaparib inhibits PARP-1 activity by 97.1% at a concentration of 1 μM in permeabilized D283Med cells.
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Fluzoparib
fluzoparib is a novel, potent, and orally available inhibitor of PARP, potentially for the treatment of solid tumours.Fluzoparib potently inhibited PARP1 enzyme activity and induced DNA double-strand breaks, G2 /M arrest, and apoptosis in homologous recombination repair (HR)-deficient cells.?
