2. Protein Tyrosine Kinase/RTK
  3. c-Fms
  4. BPR1R024

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。

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BPR1R024 Chemical Structure

BPR1R024 Chemical Structure

CAS No. : 2503015-75-4

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1 mg ￥909
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5 mg ￥2000
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25 mg ￥7000
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Customer Review

Other Forms of BPR1R024:

BPR1R024 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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[1].

IC50 & Target

IC50: 0.53 nM (CSF1R); 10 μM (AURA); 1.40 μM (AURB)[1].
体外研究
(In Vitro)

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].

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

BPR1R024 相关抗体:

Western Blot Analysis[1]

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[1].

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

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/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)[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.
分子量

482.46

Formula

C24H21F3N6O2
CAS 号
性状

固体

颜色

Off-white to light yellow

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO 中的溶解度 : 10 mg/mL (20.73 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.0727 mL 10.3636 mL 20.7271 mL
5 mM 0.4145 mL 2.0727 mL 4.1454 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: 99.06%

COA (190 KB) HNMR (142 KB) RP-HPLC (138 KB)

产品使用指南 (1538 KB)
参考文献

BPR1R024 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0727 mL 10.3636 mL 20.7271 mL 51.8178 mL
5 mM 0.4145 mL 2.0727 mL 4.1454 mL 10.3636 mL
10 mM 0.2073 mL 1.0364 mL 2.0727 mL 5.1818 mL
15 mM 0.1382 mL 0.6909 mL 1.3818 mL 3.4545 mL
20 mM 0.1036 mL 0.5182 mL 1.0364 mL 2.5909 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BPR1R0242503015-75-4c-FmsCSF-1 receptorcolony stimulating factor 1 receptorCSF-1RCSF1Roralcolony-stimulating factor-1 receptor (CSF1R)inhibitionimmuno-oncologyInhibitorinhibitorinhibit

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目录号：
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