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475949 MPS1 Inhibitor, NMS-P715 - Calbiochem

475949
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Panoramica

Replacement Information

Tabella delle specifiche principali

Empirical Formula
C₃₅H₃₉F₃N₈O₃

Products

Numero di catalogoConfezionamento Qtà/conf
475949-5MG Bottiglia di vetro 5 mg
Description
OverviewAn orally bioavailable, ATP-competitive, pyrazolo-quinazoline, MPS1 inhibitor (IC50 = 182 nM, Ki = 0.99 nM) that is shown to act in a reversible and time-dependent manner. It demonstrates selectivity for MPS1 against a panel of 60 kinases, displaying activity against only three kinases, CK2, MELK, and NEK6 (< 10 µM), 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 µM), 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. 506313).
Catalogue Number475949
Brand Family Calbiochem®
Synonyms(N-(2,6-diethylphenyl)-1-methyl-8-({4-[(1-methylpiperidin-4-yl)carbamoyl]-2-(trifluoromethoxy)phenyl}amino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide)
References
ReferencesCaldarelli, M., et al. 2011. Bioorg. Med. Chem. Lett. 21, 4507.
Colombo, R., et al. 2011. Cancer Res. 70, 10255.
Product Information
FormWhite powder
Hill FormulaC₃₅H₃₉F₃N₈O₃
Chemical formulaC₃₅H₃₉F₃N₈O₃
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
ApplicationMPS1 Inhibitor, NMS-P715, CAS 1202055-32-0, is an orally bioavailable, ATP-competitive, reversible, and time-dependent inhibitor of MPS1 (IC50 = 182 nM, Ki = 0.99 nM).
Biological Information
Purity≥98% by HPLC
Physicochemical Information
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Ambient Temperature Only
Toxicity Standard Handling
Storage +2°C to +8°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications

Documentation

MPS1 Inhibitor, NMS-P715 - Calbiochem MSDS

Titolo

Scheda di sicurezza (MSDS) 

MPS1 Inhibitor, NMS-P715 - Calbiochem Certificati d'Analisi

TitoloNumero di lotto
475949

Riferimenti bibliografici

Panoramica delle referenze
Caldarelli, M., et al. 2011. Bioorg. Med. Chem. Lett. 21, 4507.
Colombo, R., et al. 2011. Cancer Res. 70, 10255.
Scheda tecnica

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision08-June-2012 JSW
Synonyms(N-(2,6-diethylphenyl)-1-methyl-8-({4-[(1-methylpiperidin-4-yl)carbamoyl]-2-(trifluoromethoxy)phenyl}amino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide)
DescriptionAn orally bioavailable, ATP-competitive, pyrazolo-quinazoline, MPS1 inhibitor (IC50 = 182 nM, Ki>sub> = 0.99 nM) that is shown to act in a reversible and time-dependent manner. It demonstrates selectivity for MPS1 against a panel of 60 kinases, displaying activity against only three kinases, CK2, MELK, and NEK6 (< 10 µM), 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 µM), 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.
FormWhite powder
Intert gas (Yes/No) Packaged under inert gas
Chemical formulaC₃₅H₃₉F₃N₈O₃
Structure formulaStructure formula
Purity≥98% by HPLC
SolubilityDMSO (10 mg/ml; clear, colorless solution)
Storage +2°C to +8°C
Protect from light
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity Standard Handling
ReferencesCaldarelli, M., et al. 2011. Bioorg. Med. Chem. Lett. 21, 4507.
Colombo, R., et al. 2011. Cancer Res. 70, 10255.