Home Cell Cycle MPS1 inhibitor BOS172722 For research use only.

BOS172722

BOS172722 is a monopolar spindle 1 (MPS1) checkpoint inhibitor with IC50 of 11 nM, Ki of 0.11 nM.

BOS172722 Chemical Structure

BOS172722 Chemical Structure

CAS No. 1578245-44-9

Purity & Quality Control

Batch: S891101 DMSO]Insoluble]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.65%
99.65

BOS172722 Related Products

Biological Activity

Description BOS172722 is a monopolar spindle 1 (MPS1) checkpoint inhibitor with IC50 of 11 nM, Ki of 0.11 nM.
Targets
MPS1 [1]
(Cell-free assay)		 MPS1 [1]
(Cell-free assay)
0.11 nM(Ki) 11 nM
In vitro
In vitro

BOS172722 optimizes HLM stability, CDK2 selectivity, cellular potency, and solubility. BOS172722 is potential for the treatment of various forms of breast cancer.[1]
Cell Research Cell lines CAL51 cell line
Concentrations --
Incubation Time 72 h
Method

GI50 are determined using the colorimetric 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay according to manufacturer's instructions. Cells are plated in 96-well plates at 2,500 per well and treated for 72 h. The optical density is measured at 570 nm using the Wallac VICTOR2TM 1420 Multilabel Counter.
In Vivo
In vivo

BOS172722 shows excellent PK in mouse, rat, and dog. At 1 mg/kg iv and 5 mg/kg po, BOS172722 shows complete bioavailability (100%), low clearance (1.2 mL/min/kg), a moderate volume of distribution (1.1 L/kg), and a 12 h half-life in a dog PK study. The 50 mg/kg dose of BOS172722 results in an increased suppression of MPS1 autophosphorylation at 6 and 24 h.[1]
Animal Research Animal Models Dog, mouse, rat
Dosages 1 mg/kg, 5 mg/kg, 2.5 mg/kg
Administration IV, PO
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03328494 Completed
Advanced Nonhaematologic Malignancies
Boston Pharmaceuticals
 October 13 2017 Phase 1

Chemical Information & Solubility

Molecular Weight 446.55 Formula

C24H30N8O
CAS No. 1578245-44-9 SDF --
Smiles CCOC1=C(C=CC(=C1)C2=NN=CN2C)NC3=NC=C4C=C(N=C(C4=N3)NCC(C)(C)C)C
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : Insoluble ( Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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