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MedKoo Cat#: 406380 | Name: NMS-P715
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

NMS-P715 is a selective and orally bioavailable MPS1 inhibitor, which selectively reduces cancer cell proliferation, leaving normal cells almost unaffected. NMS-P715 accelerates mitosis and affects kinetochore components localization causing massive aneuploidy and cell death in a variety of tumoral cell lines and inhibits tumor growth in preclinical cancer models. Inhibiting the SAC could represent a promising new approach to selectively target cancer cells.

Chemical Structure

NMS-P715
NMS-P715
CAS#1202055-34-2

Theoretical Analysis

MedKoo Cat#: 406380

Name: NMS-P715

CAS#: 1202055-34-2

Chemical Formula: C35H39F3N8O3

Exact Mass: 676.3097

Molecular Weight: 676.75

Elemental Analysis: C, 62.12; H, 5.81; F, 8.42; N, 16.56; O, 7.09

Price and Availability

Size Price Availability Quantity
5mg USD 400.00 2 Weeks
10mg USD 750.00 2 Weeks
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Related CAS #
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Synonym
NMSP715; NMSP715; NMSP715; NMSP 715.
IUPAC/Chemical Name
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
InChi Key
JFOAJUGFHDCBJJ-UHFFFAOYSA-N
InChi Code
InChI=1S/C35H39F3N8O3/c1-5-20-8-7-9-21(6-2)28(20)42-33(48)30-25-12-10-23-19-39-34(43-29(23)31(25)46(4)44-30)41-26-13-11-22(18-27(26)49-35(36,37)38)32(47)40-24-14-16-45(3)17-15-24/h7-9,11,13,18-19,24H,5-6,10,12,14-17H2,1-4H3,(H,40,47)(H,42,48)(H,39,41,43)
SMILES Code
O=C(C1=NN(C)C2=C1CCC3=CN=C(NC4=CC=C(C(NC5CCN(C)CC5)=O)C=C4OC(F)(F)F)N=C23)NC6=C(CC)C=CC=C6CC
Appearance
solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO, not in water
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
  NMS-P715 limits tumor growth in xenograft models. In cancer cell lines, NMS-P715 causes cell death associated with impaired SAC function and increased chromosome mis-segregation. NMS-P715 could have a favorable therapeutic index and warrant further investigation of MPS1 inhibition as a new PDAC treatment strategy.       
Product Data
Product Data
Instruction
View handling instruction
Biological target:
NMS-P715 is a selective and orally bioavailable MPS1 inhibitor.
In vitro activity:
This study provides new evidence that NMS-P715 potently inhibited cell proliferation and colony formation in both CCA cell lines. The recent study showed that NMS-P715 activated caspase-dependent apoptosis and autophagosome formation with an increase of LC3 A/B-II protein expression in CCA cell lines. NMS-P715 also greatly impeded cell migration and invasion in CCA cell lines. Reference: Eur J Pharmacol. 2022 May 5;922:174899. https://pubmed.ncbi.nlm.nih.gov/35337815/
In vivo activity:
NMS-P715 accelerates mitosis and affects kinetochore components localization causing massive aneuploidy and cell death in a variety of tumoral cell lines and inhibits tumor growth in preclinical mouse cancer models. Reference: Cancer Res. 2010 Dec 15;70(24):10255-64. https://pubmed.ncbi.nlm.nih.gov/21159646/

Preparing Stock Solutions

The following data is based on the product molecular weight 676.75 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Waenphimai O, Mahalapbutr P, Vaeteewoottacharn K, Wongkham S, Sawanyawisuth K. Multiple actions of NMS-P715, the monopolar spindle 1 (MPS1) mitotic checkpoint inhibitor in liver fluke-associated cholangiocarcinoma cells. Eur J Pharmacol. 2022 May 5;922:174899. doi: 10.1016/j.ejphar.2022.174899. Epub 2022 Mar 23. PMID: 35337815. 2. Maachani UB, Kramp T, Hanson R, Zhao S, Celiku O, Shankavaram U, Colombo R, Caplen NJ, Camphausen K, Tandle A. Targeting MPS1 Enhances Radiosensitization of Human Glioblastoma by Modulating DNA Repair Proteins. Mol Cancer Res. 2015 May;13(5):852-62. doi: 10.1158/1541-7786.MCR-14-0462-T. Epub 2015 Feb 26. PMID: 25722303; PMCID: PMC4433451. 3. Slee RB, Grimes BR, Bansal R, Gore J, Blackburn C, Brown L, Gasaway R, Jeong J, Victorino J, March KL, Colombo R, Herbert BS, Korc M. Selective inhibition of pancreatic ductal adenocarcinoma cell growth by the mitotic MPS1 kinase inhibitor NMS-P715. Mol Cancer Ther. 2014 Feb;13(2):307-315. doi: 10.1158/1535-7163.MCT-13-0324. Epub 2013 Nov 26. PMID: 24282275; PMCID: PMC4217310. 4. Colombo R, Caldarelli M, Mennecozzi M, Giorgini ML, Sola F, Cappella P, Perrera C, Depaolini SR, Rusconi L, Cucchi U, Avanzi N, Bertrand JA, Bossi RT, Pesenti E, Galvani A, Isacchi A, Colotta F, Donati D, Moll J. Targeting the mitotic checkpoint for cancer therapy with NMS-P715, an inhibitor of MPS1 kinase. Cancer Res. 2010 Dec 15;70(24):10255-64. doi: 10.1158/0008-5472.CAN-10-2101. PMID: 21159646.
In vitro protocol:
1. Waenphimai O, Mahalapbutr P, Vaeteewoottacharn K, Wongkham S, Sawanyawisuth K. Multiple actions of NMS-P715, the monopolar spindle 1 (MPS1) mitotic checkpoint inhibitor in liver fluke-associated cholangiocarcinoma cells. Eur J Pharmacol. 2022 May 5;922:174899. doi: 10.1016/j.ejphar.2022.174899. Epub 2022 Mar 23. PMID: 35337815. 2. Maachani UB, Kramp T, Hanson R, Zhao S, Celiku O, Shankavaram U, Colombo R, Caplen NJ, Camphausen K, Tandle A. Targeting MPS1 Enhances Radiosensitization of Human Glioblastoma by Modulating DNA Repair Proteins. Mol Cancer Res. 2015 May;13(5):852-62. doi: 10.1158/1541-7786.MCR-14-0462-T. Epub 2015 Feb 26. PMID: 25722303; PMCID: PMC4433451.
In vivo protocol:
1. Slee RB, Grimes BR, Bansal R, Gore J, Blackburn C, Brown L, Gasaway R, Jeong J, Victorino J, March KL, Colombo R, Herbert BS, Korc M. Selective inhibition of pancreatic ductal adenocarcinoma cell growth by the mitotic MPS1 kinase inhibitor NMS-P715. Mol Cancer Ther. 2014 Feb;13(2):307-315. doi: 10.1158/1535-7163.MCT-13-0324. Epub 2013 Nov 26. PMID: 24282275; PMCID: PMC4217310. 2. Colombo R, Caldarelli M, Mennecozzi M, Giorgini ML, Sola F, Cappella P, Perrera C, Depaolini SR, Rusconi L, Cucchi U, Avanzi N, Bertrand JA, Bossi RT, Pesenti E, Galvani A, Isacchi A, Colotta F, Donati D, Moll J. Targeting the mitotic checkpoint for cancer therapy with NMS-P715, an inhibitor of MPS1 kinase. Cancer Res. 2010 Dec 15;70(24):10255-64. doi: 10.1158/0008-5472.CAN-10-2101. PMID: 21159646.
1: Slee RB, Grimes BR, Bansal R, Gore J, Blackburn C, Brown L, Gasaway R, Jeong J, Victorino J, March KL, Colombo R, Herbert BS, Korc M. Selective inhibition of pancreatic ductal adenocarcinoma cell growth by the mitotic MPS1 kinase inhibitor, NMS-P715. Mol Cancer Ther. 2013 Nov 26. [Epub ahead of print] PubMed PMID: 24282275. 2: Colombo R, Caldarelli M, Mennecozzi M, Giorgini ML, Sola F, Cappella P, Perrera C, Depaolini SR, Rusconi L, Cucchi U, Avanzi N, Bertrand JA, Bossi RT, Pesenti E, Galvani A, Isacchi A, Colotta F, Donati D, Moll J. Targeting the mitotic checkpoint for cancer therapy with NMS-P715, an inhibitor of MPS1 kinase. Cancer Res. 2010 Dec 15;70(24):10255-64. doi: 10.1158/0008-5472.CAN-10-2101. PubMed PMID: 21159646.