BOS172722

Catalog No.S8911

For research use only.

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

BOS172722 Chemical Structure

CAS No. 1578245-44-9

Purity & Quality Control

Choose Selective MPS1 Inhibitors

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

BOS172722 optimizes HLM stability, CDK2 selectivity, cellular potency, and solubility. BOS172722 is potential for the treatment of various forms of breast cancer.[1]

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]

Protocol (from reference)

Cell Research:

[1]

  • 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.

  • (Only for Reference)
Animal Research:

[1]

  • Animal Models: Dog, mouse, rat
  • Dosages: 1 mg/kg, 5 mg/kg, 2.5 mg/kg
  • Administration: IV, PO
  • (Only for Reference)

Solubility (25°C)

In vitro

DMSO 89 mg/mL
(199.3 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 446.55
Formula

C24H30N8O

CAS No. 1578245-44-9
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCOC1=C(C=CC(=C1)C2=NN=CN2C)NC3=NC=C4C=C(N=C(C4=N3)NCC(C)(C)C)C

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03328494 Completed Drug: BOS172722|Drug: Paclitaxel Advanced Nonhaematologic Malignancies Boston Pharmaceuticals October 13 2017 Phase 1

(data from https://clinicaltrials.gov, updated on 2021-09-06)

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

Tel: +1-832-582-8158 Ext:3
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