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506313 InSolution™ MPS1 Inhibitor, NMS-P715 - Calbiochem

A 5 mM (2 mg/592 µl) sterile-filtered solution of MPS1 Inhibitor, NMS-P715 in DMSO.

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: N-(2,6-Diethylphenyl)-1-methyl-8-((4-(1-methylpiperidin-4-yl)carbamoyl)-2-(trifluoromethoxy)phenylamino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide, MPS1 Inhibitor, NMS-P715 InSolution

Primary Target: MPS1
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Overview

Replacement Information

Key Spec Table

Empirical Formula
C₃₅H₃₉F₃N₈O₃
Description
Overview

This product has been discontinued.
Catalogue Number506313
Brand Family Calbiochem®
SynonymsN-(2,6-Diethylphenyl)-1-methyl-8-((4-(1-methylpiperidin-4-yl)carbamoyl)-2-(trifluoromethoxy)phenylamino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide, MPS1 Inhibitor, NMS-P715 InSolution
References
ReferencesCaldarelli, M., et al. 2011. Bioorg. Med. Chem. Lett. 21, 4507.
Colombo, R., et al. 2011. Cancer Res. 70, 10255.
Product Information
FormLiquid
FormulationA 5 mM (2 mg/592 µl) sterile-filtered solution of MPS1 Inhibitor, NMS-P715 (Cat. No. 475949) in DMSO.
Hill FormulaC₃₅H₃₉F₃N₈O₃
Chemical formulaC₃₅H₃₉F₃N₈O₃
Hygroscopic Hygroscopic
ReversibleY
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Primary TargetMPS1
Purity≥98% by HPLC
Physicochemical Information
Cell permeableY
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Dry Ice Only
Toxicity Standard Handling
Storage ≤ -70°C
Protect from Light Protect from light
Hygroscopic Hygroscopic
Avoid freeze/thaw Avoid freeze/thaw
Do not freeze Ok to freeze
Special InstructionsFollowing initial thaw, aliquot and freeze (-20°C). Aliquots are stable for up to 6 months at -20°C. If necessary, slightly warm the vial. Use only fresh DMSO for further dilutions prior to use.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Catalogue Number GTIN
506313 0

Documentation

InSolution™ MPS1 Inhibitor, NMS-P715 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

References

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

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.

Revision11-July-2014 JSW
SynonymsN-(2,6-Diethylphenyl)-1-methyl-8-((4-(1-methylpiperidin-4-yl)carbamoyl)-2-(trifluoromethoxy)phenylamino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide, MPS1 Inhibitor, NMS-P715 InSolution
DescriptionAn 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.
FormLiquid
FormulationA 5 mM (2 mg/592 µl) sterile-filtered solution of MPS1 Inhibitor, NMS-P715 (Cat. No. 475949) in DMSO.
Intert gas (Yes/No) Packaged under inert gas
Chemical formulaC₃₅H₃₉F₃N₈O₃
Structure formulaStructure formula
Purity≥98% by HPLC
Storage Protect from light
Avoid freeze/thaw
≤ -70°C
Hygroscopic
Do Not Freeze Ok to freeze
Special InstructionsFollowing initial thaw, aliquot and freeze (-20°C). Aliquots are stable for up to 6 months at -20°C. If necessary, slightly warm the vial. Use only fresh DMSO for further dilutions prior to use.
Toxicity Standard Handling
ReferencesCaldarelli, M., et al. 2011. Bioorg. Med. Chem. Lett. 21, 4507.
Colombo, R., et al. 2011. Cancer Res. 70, 10255.