BPR1R024

• CAT Number: I045328
• CAS Number: 2503015-75-4
• Molecular Formula: C24H21F3N6O2
• Molecular Weight: 482.46
• Purity: ≥95%
• Synonyms: 1-[4-[7-(dimethylamino)quinazolin-4-yl]oxyphenyl]-3-[[6-(trifluoromethyl)pyridin-3-yl]methyl]urea
• InChI: InChI=1S/C24H21F3N6O2/c1-33(2)17-6-9-19-20(11-17)30-14-31-22(19)35-18-7-4-16(5-8-18)32-23(34)29-13-15-3-10-21(28-12-15)24(25,26)27/h3-12,14H,13H2,1-2H3,(H2,29,32,34)
• InChIKey: ORYMWWSJZRCUSV-UHFFFAOYSA-N
• SMILES: CN(C)C1=CC2=C(C=C1)C(=NC=N2)OC3=CC=C(C=C3)NC(=O)NCC4=CN=C(C=C4)C(F)(F)F

BPR1R024 (Cat No.: I045328) is a potent, orally bioavailable small-molecule antagonist of CSF1R (colony-stimulating factor‑1 receptor), with biochemical potency of ~0.53 nM. It selectively inhibits protumor M2-like tumor-associated macrophage (TAM) survival while sparing M1-like anti-tumor macrophages, showing minimal off-target activity (AURKA/B IC₅₀ >1 µM). In murine MC38 colon‐cancer models, oral administration (100 mg/kg twice daily) significantly delayed tumor growth and reshaped the immunosuppressive microenvironment by increasing the M1/M2 ratio, indicating notable immunomodulatory and antitumor efficacy.

Reference

[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.
[Content Brief]