2503015-75-4

Name	Urea, N-[4-[[7-(dimethylamino)-4-quinazolinyl]oxy]phenyl]-N'-[[6-(trifluoromethyl)-3-pyridinyl]methyl]-
CAS	2503015-75-4
Molecular Formula	C24H21F3N6O2
Molecular Weight	482.46
MOL File	2503015-75-4.mol

Synonyms

BPR1R024 Urea, N-[4-[[7-(dimethylamino)-4-quinazolinyl]oxy]phenyl]-N'-[[6-(trifluoromethyl)-3-pyridinyl]methyl]-

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Chemical Properties

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

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/mLh by the IV route and 362 ng/mLh 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

Supplier

Shanghai finete Pharmaceutical Co., Ltd.

Telephone021-021-00000000 18221039705

Websitehttp://www.finetechpharm.cn

TargetMol Chemicals Inc.

Telephone 4008200310

Websitehttps://www.targetmol.cn/

Shanghai Yifei Biotechnology Co. , Ltd.

Telephone021-65675885 18964387627

Websitehttp://www.efebio.com

Shanghai?Medlife?Pharm-Tech?Co.,?Ltd

Telephone021-59167510 18117107507

Websitehttps://www.med-life.cn/

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