| Identification | Back Directory | [Name]
Urea, N-[4-[[7-(dimethylamino)-4-quinazolinyl]oxy]phenyl]-N'-[[6-(trifluoromethyl)-3-pyridinyl]methyl]- | [CAS]
2503015-75-4 | [Synonyms]
BPR1R024
Urea, N-[4-[[7-(dimethylamino)-4-quinazolinyl]oxy]phenyl]-N'-[[6-(trifluoromethyl)-3-pyridinyl]methyl]- | [Molecular Formula]
C24H21F3N6O2 | [MOL File]
2503015-75-4.mol | [Molecular Weight]
482.46 |
| Chemical Properties | Back Directory | [Boiling point ]
621.3±55.0 °C(Predicted) | [density ]
1.386±0.06 g/cm3(Predicted) | [form ]
Solid | [pka]
12.33±0.46(Predicted) | [color ]
Off-white to light yellow |
| Hazard Information | Back Directory | [Uses]
BPR1R024 is an orally active and selective colony-stimulating factor-1 receptor (CSF1R) inhibitor. BPR1R024 has potent CSF1R inhibition activity with an IC50 value of 0.53 nM. BPR1R024 can be used for the research of immuno-oncology[1]. | [in vivo]
BPR1R024 (compound 12) (oral; 100 mg/kg; twice a day) exhibits antitumor and immunomodulatory activity in a murine colon tumor model[1]. | Animal Model: | Rats[1] | | Dosage: | 5, 20, 25 mg/kg | | Administration: | IV, PO | | Result: | Exhibited high systemic drug exposure with the dose-normalized area under curve (DNAUC) values of 3635 ng/mL*h by the IV route and 362 ng/mL*h by the PO route and the modification increased oral bioavailability (F=35%). |
| Animal Model: | C57BL/6 mice (six-week-old, male)[1] | | Dosage: | 100 mg/kg | | Administration: | Oral, twice a day | | Result: | Delayed the MC38 murine colon tumor growth and reversed the immunosuppressive tumor microenvironment with the increased M1/M2 ratio. |
| [References]
[1] Lee KH, et al. Discovery of BPR1R024, an Orally Active and Selective CSF1R Inhibitor that Exhibits Antitumor and Immunomodulatory Activity in a Murine Colon Tumor Model. J Med Chem. 2021 Oct 14;64(19):14477-14497. DOI:10.1021/acs.jmedchem.1c01006 |
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| Company Name: |
BOC Sciences
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1-631-485-4226; 16314854226 |
| Website: |
https://www.bocsci.com |
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