产品
编 号：F753436
分子式：C24H21F3N6O2
分子量：482.46
分子式：C24H21F3N6O2
分子量：482.46
产品类型
规格
价格
是否有货
1mg
询价
询价
5mg
询价
询价
10mg
询价
询价
25mg
询价
询价
结构图
CAS No: 2503015-75-4
产品详情
生物活性：
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.
体内研究：
BPR1R024 (compound 12) (oral; 100 mg/kg; twice a day) exhibits antitumor and immunomodulatory activity in a murine colon tumor model.Animal Model:Rats
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)
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.
体外研究：
BPR1R024 (compound 12) has potent CSF1R inhibition activity with an IC50 value of 0.53 nM.BPR1R024 exhibits weake AURA and AURB inhibitory activity inenzyme activity assay with IC50 values of ＞10 μM and 1.40 μM, respeactively.BPR1R024 (0-500 nM) significantly suppressed the CSF1R signal in a dose-dependent manner.BPR1R024 (10 nM, 100 nM) inhibits CSF1/CSF1R signaling-mediated TNF-α production.BPR1R024 (0-10 μM) specifically inhibits protumor M2-like macrophage survival with a minimal effect on antitumor M1-like macrophage growth.
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.
体内研究：
BPR1R024 (compound 12) (oral; 100 mg/kg; twice a day) exhibits antitumor and immunomodulatory activity in a murine colon tumor model.Animal Model:Rats
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)
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.
体外研究：
BPR1R024 (compound 12) has potent CSF1R inhibition activity with an IC50 value of 0.53 nM.BPR1R024 exhibits weake AURA and AURB inhibitory activity inenzyme activity assay with IC50 values of ＞10 μM and 1.40 μM, respeactively.BPR1R024 (0-500 nM) significantly suppressed the CSF1R signal in a dose-dependent manner.BPR1R024 (10 nM, 100 nM) inhibits CSF1/CSF1R signaling-mediated TNF-α production.BPR1R024 (0-10 μM) specifically inhibits protumor M2-like macrophage survival with a minimal effect on antitumor M1-like macrophage growth.
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