BPR1R024 mesylate_product_DataBase

Bioactivity	BPR1R024 mesylate is an orally active and selective colony-stimulating factor-1 receptor (CSF1R) inhibitor.BPR1R024 mesylate is the equivalent of BPR1R024 (HY-132935). 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].
Target	IC50: 0.53 nM (CSF1R); 10 μM (AURA); 1.40 μM (AURB).
Invitro	BPR1R024 (compound 12) has potent CSF1R inhibition activity with an IC50 value of 0.53 nM[1].BPR1R024 exhibits weake AURA and AURB inhibitory activity in enzyme activity assay with IC50 values of ＞10 μM and 1.40 μM, respeactively[1].BPR1R024 (0-500 nM) significantly suppressed the CSF1R signal in a dose-dependent manner[1].BPR1R024 (10 nM, 100 nM) inhibits CSF1/CSF1R signaling-mediated TNF-α production[1].BPR1R024 (0-10 μM) specifically inhibits protumor M2-like macrophage survival with a minimal effect on antitumor M1-like macrophage growth[1]. Western Blot Analysis[1] Cell Line:
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:
Name	BPR1R024 mesylate
CAS	2763365-40-6
Formula	C25H25F3N6O5S
Molar Mass	578.56
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[1]. Kun-Hung Lee, 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.

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BPR1R024 mesylate

CAS: 2763365-40-6 F: C25H25F3N6O5S W: 578.56