Synonym
MpsBAY2a; Mps-BAY-2a; Mps BAY 2a;
IUPAC/Chemical Name
N-Cyclopropyl-4-[8-[(2-methylpropyl)amino]-6-(5-quinolinyl)imidazo[1,2-a]pyrazin-3-yl]benzamide
InChi Key
MDYKTGNHXNTATG-UHFFFAOYSA-N
InChi Code
InChI=1S/C29H28N6O/c1-18(2)15-31-27-28-32-16-26(19-8-10-20(11-9-19)29(36)33-21-12-13-21)35(28)17-25(34-27)23-5-3-7-24-22(23)6-4-14-30-24/h3-11,14,16-18,21H,12-13,15H2,1-2H3,(H,31,34)(H,33,36)
SMILES Code
O=C(NC1CC1)C2=CC=C(C3=CN=C4C(NCC(C)C)=NC(C5=C6C=CC=NC6=CC=C5)=CN43)C=C2
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
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
Biological target:
Mps-BAY2a is a monopolar spindle 1 (MPS1) inhibitor with an IC50 of 1 nM against human MPS1.
In vitro activity:
Cancer cells treated with Mps-BAY1 or Mps-BAY2a manifested multiple signs of mitotic perturbation including inefficient chromosomal congression during metaphase, unscheduled SAC inactivation and severe anaphase defects. Videomicroscopic cell fate profiling of histone 2B-green fluorescent protein-expressing cells revealed the capacity of MPS1 inhibitors to subvert the correct timing of mitosis as they induce a premature anaphase entry in the context of misaligned metaphase plates. Hence, in the presence of MPS1 inhibitors, cells either divided in a bipolar (but often asymmetric) manner or entered one or more rounds of abortive mitoses, generating gross aneuploidy and polyploidy, respectively.
Reference: Cell Death Differ. 2013 Nov;20(11):1532-45. https://pubmed.ncbi.nlm.nih.gov/23933817/
|
Solvent |
mg/mL |
mM |
| Solubility |
| DMSO |
10.0 |
20.98 |
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.
Preparing Stock Solutions
The following data is based on the
product
molecular weight
476.58
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.
| 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:
Jemaà M, Galluzzi L, Kepp O, Senovilla L, Brands M, Boemer U, Koppitz M, Lienau P, Prechtl S, Schulze V, Siemeister G, Wengner AM, Mumberg D, Ziegelbauer K, Abrieu A, Castedo M, Vitale I, Kroemer G. Characterization of novel MPS1 inhibitors with preclinical anticancer activity. Cell Death Differ. 2013 Nov;20(11):1532-45. doi: 10.1038/cdd.2013.105. Epub 2013 Aug 9. PMID: 23933817; PMCID: PMC3792427.
In vitro protocol:
Jemaà M, Galluzzi L, Kepp O, Senovilla L, Brands M, Boemer U, Koppitz M, Lienau P, Prechtl S, Schulze V, Siemeister G, Wengner AM, Mumberg D, Ziegelbauer K, Abrieu A, Castedo M, Vitale I, Kroemer G. Characterization of novel MPS1 inhibitors with preclinical anticancer activity. Cell Death Differ. 2013 Nov;20(11):1532-45. doi: 10.1038/cdd.2013.105. Epub 2013 Aug 9. PMID: 23933817; PMCID: PMC3792427.
1: Jemaà M, Galluzzi L, Kepp O, Senovilla L, Brands M, Boemer U, Koppitz M, Lienau P, Prechtl S, Schulze V, Siemeister G, Wengner AM, Mumberg D, Ziegelbauer K, Abrieu A, Castedo M, Vitale I, Kroemer G. Characterization of novel MPS1 inhibitors with preclinical anticancer activity. Cell Death Differ. 2013 Nov;20(11):1532-45. doi: 10.1038/cdd.2013.105. Epub 2013 Aug 9. PubMed PMID: 23933817; PubMed Central PMCID: PMC3792427.
