475949

NMS-P715

≥98% (HPLC), powder, MPS1 inhibitor, Calbiochem^®

• Synonym(e): MPS1-Inhibitor, NMS-P715, (N-(2,6-Diethylphenyl)-1-Methyl-8-({4-[(1-Methylpiperidin-4-yl)Carbamoyl]-2-(Trifluormethoxy)phenyl}amino)-4,5-Dihydro-1H-Pyrazol[4,3-h]Chinazolin-3-Carboxamid)
• Empirische Formel (Hill-System): C₃₅H₃₉F₃N₈O₃
• CAS-Nummer: 1202055-32-0
• Molekulargewicht: 676.73
• UNSPSC Code: 12352200
• NACRES: NA.77
• MDL number: MFCD19443684
• Assay: ≥98% (HPLC)
• Form: powder
• Quality level: 100
• Storage condition: OK to freeze, protect from light

Eigenschaften

• Produktname: MPS1-Inhibitor, NMS-P715, The MPS1 Inhibitor, NMS-P715 controls the biological activity of MPS1. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.
• Quality Level: 100
• assay: ≥98% (HPLC)
• form: powder
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze, protect from light
• color: white
• solubility: DMSO: 10 mg/mL, clear, colorless
• shipped in: ambient
• storage temp.: 2-8°C
• SMILES string: CN(N=C1C(NC2=C(CC)C=CC=C2CC)=O)C3=C1CCC4=C3N=C(NC5=CC=C(C(NC6CCN(C)CC6)=O)C=C5OC(F)(F)F)N=C4
• InChI key: JFOAJUGFHDCBJJ-UHFFFAOYSA-N

Beschreibung

General description

Ein oral bioverfügbarer, ATP-kompetitiver Pyrazolchinazolin-MPS1-Inhibitor (IC₅₀ = 182 nM, K_i = 0,99 nM), der nachweislich reversibel und zeitabhängig wirkt. Er zeigt Selektivität für MPS1 gegenüber einer Gruppe von 60 Kinasen, wobei er nur gegen die drei Kinasen CK2, MELK und NEK6 wirkt (<10 M), but not against other mitotic kinases including PLK1, CDK1, Aurora A, Aurora B, or the SAC kinase BUB1, in an in vitro kinase assay. It promotes massive SAC (spindle assembly checkpoint) override (EC₅₀ = 65 nM) in nocodazole-arrested U20S cells and elicits a reduction in the G1 and G2/M phase of the cell cycle in A2780 ovarian cancer cells, similar to RNAi-mediated MPS1 silencing. In addition, it is shown to inactivate SAC, delocalize kinetochore components, and inhibit the proliferation of select cancer cell lines (IC₅₀ ~ 1 M), without marked activity among a panel of 127 normal cell lines. Also, it inhibits A2780 tumor xenograft growth in mice (90 mg/kg/day, o.s., in vivo) by 53% without marked body weight loss. Also available as a 5 mM solution in DMSO (Cat. No. 5.06313).

Packaging

Verpackt unter inertem Gas

Preparation Note

Nach der Rekonstitution in Aliquote aufteilen und einfrieren (-20 °;C). Stammlösungen sind bei -20 °;C bis zu 3 Monate haltbar.

Other Notes

Caldarelli, M., et al. 2011. Bioorg. Med. Chem. Lett.21, 4507.
Colombo, R., et al. 2011. Cancer Res.70, 10255.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxizität: Standard-Handhabung (A)

Sicherheitshinweise

• Lagerklasse: 11 - Combustible Solids
• wgk: WGK 2
• flash_point_f: Not applicable
• flash_point_c: Not applicable