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Purity: ≥98%
BOS172722 is a novel, potent and selective inhibitor of monopolar spindle 1 (MPS1) with IC50 of 2-11 nM. BOS172722 showed high bioavailability in all three species despite very modest solubility at physiological pH. MPS1 occupies a central role in mitosis and is one of the main components of the spindle assembly checkpoint. The MPS1 kinase is an attractive cancer target.
| ln Vitro |
BOS-172722 has an IC50 of 2 nM and is a monopolar spindle 1 (MPS1) checkpoint equivalent. Additionally, BOS-172722 may be able to treat different types of breast cancer [1].
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| ln Vivo |
Excellent pharmacokinetic activity of BOS-172722 has been observed in mice, adsorbents, and dogs [1]. At 6 and 24 hours, BOS-172722 (50 mg/kg) causes an increase in MPS1 autophosphorylation adsorption [1].
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| Animal Protocol |
Animal/Disease Models: dog [2]. 1].
Doses: 1 mg/kg (intravenous (iv) (iv)injection), 5 mg/kg (oral) (pharmacokinetic/PK/PK analysis). Doses: IV and PO. Experimental Results: T1/2 = 12 hrs (hrs (hours)), Cmaxpo = 7770 nmol/L, AUCpo = 147035 h*nmol/L. |
| References | |
| Additional Infomation |
BOS172722 is a novel and selective Monopolar spindle 1 (Mps1) kinase inhibitor identified as a potential anticancer agent. Normally, Mps1 supports the proper division of cancer cells, ensuring survival and replication. The key role of Mps1 in the growth of cancer cells renders it an appealing target for cancer treatment, as its inhibition could lead to favorable effects. An in vivo study combined BOS172722 with [Paclitaxel] for the treatment of triple hormone receptor negative breast cancer, and demonstrated promising synergistic effects.
Mps1 Inhibitor BOS172722 is an orally bioavailable, selective inhibitor of the serine/threonine-protein kinase monopolar spindle 1 (Mps1; TTK), with potential antineoplastic activity. Upon administration, the Mps1 inhibitor BOS172722 binds to and inhibits the activity of Mps1, a core component of the spindle assembly checkpoint (SAC). Inhibition of Mps1 activity compromises spindle assembly checkpoint, increases chromosome missegregation errors and decreases cancer cell viability. Mps1, a dual-specificity protein kinase expressed in proliferating normal tissues and aberrantly overexpressed in certain tumor types, is activated during mitosis and is essential in proper SAC function and chromosomal alignment. Mechanism of Action Mps1 is a protein kinase that is expressed in normal proliferating tissues and in certain actively dividing tumors. It acts during mitosis (cell division) and plays a crucial role in the alignment of chromosomes in cancer cells. Checkpoint activities by Mps1 normally inhibit the advancement of cancer cells from metaphase to anaphase until structural integrity and alignment occur. BOS172722 binds to Mps1, inhibiting its regulatory checkpoint activities. This inhibition causes accelerated cell division with increased missegregation errors that ultimately reduce the viability of malignant cells. |
| Molecular Formula |
C24H30N8O
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|---|---|
| Molecular Weight |
446.548003673553
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| Exact Mass |
446.25
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| Elemental Analysis |
C, 64.55; H, 6.77; N, 25.09; O, 3.58
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| CAS # |
1578245-44-9
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| PubChem CID |
73386890
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
4.3
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
33
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| Complexity |
616
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
SGWLRDAOCLITOM-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H30N8O/c1-7-33-19-11-16(22-31-27-14-32(22)6)8-9-18(19)29-23-25-12-17-10-15(2)28-21(20(17)30-23)26-13-24(3,4)5/h8-12,14H,7,13H2,1-6H3,(H,26,28)(H,25,29,30)
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| Chemical Name |
N2-(2-ethoxy-4-(4-methyl-4H-1,2,4-triazol-3-yl)phenyl)-6-methyl-N8-neopentylpyrido[3,4-d]pyrimidine-2,8-diamine
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| Synonyms |
BOS172722 BOS-172722 BOS 172722
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
1M HCl : 65 mg/mL (~145.56 mM)
DMSO : ~5 mg/mL (~11.20 mM) |
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2394 mL | 11.1970 mL | 22.3939 mL | |
| 5 mM | 0.4479 mL | 2.2394 mL | 4.4788 mL | |
| 10 mM | 0.2239 mL | 1.1197 mL | 2.2394 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT03328494 | COMPLETED | Drug: BOS172722 Drug: Paclitaxel |
Advanced Nonhaematologic Malignancies | Boston Pharmaceuticals | 2017-10-13 | Phase 1 |
| NCT03464058 | COMPLETED | Drug: BOS172767 tablets Drug: BOS172767 liquid capsules Drug: BOS172767 micronized capsules |
Healthy Subjects | Boston Pharmaceuticals | 2018-03-21 | Phase 1 |
Products are for research use only; We do not sell to patients
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