BPR1R024|cas:2503015-75-4|西域试剂

BPR1R024,99.06%

产品编号：Bellancom-132935| CAS NO：2503015-75-4| 分子式：C₂₄H₂₁F₃N₆O₂| 分子量：482.46

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-132935	￥2000.00	杭州北京（现货）
Bellancom-132935	￥3500.00	杭州北京（现货）
Bellancom-132935	￥7000.00	杭州北京（现货）
Bellancom-132935	￥11000.00	杭州北京（现货）

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BPR1R024

产品介绍

BPR1R024 是一种选择性的集落刺激因子-1 受体(CSF1R) 抑制剂，具有口服活性。BPR1R024 具有有效的 CSF1R 抑制活性，IC₅₀ 值为 0.53 nM。BPR1R024 可用于免疫肿瘤学研究。

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 in enzyme 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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis

Cell Line:	RAW264.7 and THP-1 cells
Concentration:	0-500 nM
Incubation Time:	16 h
Result:	Significantly suppressed the CSF1R signal in a dose-dependent manner, at concentrations of approximately 50-75 and 1-10 nM in RAW264.7 and THP-1 cells, respectively.

体内研究
(In Vivo)

BPR1R024 (compound 12) (oral; 100 mg/kg; twice a day) exhibits antitumor and immunomodulatory activity in a murine colon tumor model.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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/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)
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.

体内研究

BPR1R024 (compound 12) (oral; 100 mg/kg; twice a day) exhibits antitumor and immunomodulatory activity in a murine colon tumor model.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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/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)
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.

体内研究

BPR1R024 (compound 12) (oral; 100 mg/kg; twice a day) exhibits antitumor and immunomodulatory activity in a murine colon tumor model.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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/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)
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.