1. Protein Tyrosine Kinase/RTK
  2. c-Fms
  3. CSF1R-IN-15

CSF1R-IN-15 (compound 23) 是 c-Fms 的抑制剂。集落刺激因子-1受体 (c-Fms) 是一种嵌入巨噬细胞细胞膜的酪氨酸激酶。该受体被集落刺激因子-1 (CSF1) 和白细胞介素-34 激活,通过 CSF1R 信号传导对巨噬细胞的分化、增殖和存活至关重要。

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CSF1R-IN-15 Chemical Structure

CSF1R-IN-15 Chemical Structure

CAS No. : 2925744-43-8

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CSF1R-IN-15 (compound 23) is an inhibitor targeting CSF1R. The colony-stimulating factor-1 receptor (CSF1R) is a tyrosine kinase embedded in the cell membrane of macrophages. The receptor is activated by colony-stimulating factor-1 (CSF-1) and interleukin-34, and signaling via CSF1R is crucial for the differentiation, proliferation, and survival of macrophages[1].

体外研究
(In Vitro)

CSF1R-IN-15 (0.007-10 μM, 72 h) 对 Ba/F3 细胞没有活性,而 pexidartinib (HY-16749) 具有优越的活性[1]
CSF1R-IN-15 对血浆蛋白结合的评估是通过平衡透析法进行的。CSF1R-IN-15 (5 μM, 6 h, 37 °C) 与血浆孵化,与小鼠血浆蛋白结合率为 69%[1]

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

Cell Viability Assay[1]

Cell Line: Ba/F3-hCSF1R Cells
Concentration: 0.007-10 μM
Incubation Time: 72 h
Result: Exhibited no activity while pexidartinib (HY-16749) has superior activity.
体内研究
(In Vivo)

CSF1R-IN-15 体内药代动力学指标来自于盒式给药研究。CSF1R-IN-15 在 C57BLKS 小鼠中的 t1/2,C0,AUC0-∞,CLobs 和 Vss,obs 分别为 0.5 h,37 ng/ml,18 h*ng/ml,54 L/h/kg 和 32 L/k[1]

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

Animal Model: In Vivo Pharmacokinetic Study
Dosage: 1mg/kg
Administration: Intravenous injection (i.v.) single dosing of drugs (1 mg/kg each) in a 20% DMSO, 80% PEG400 formulation. Blood sampling was done after 10, 30, 60, 120, 240, and 480 min.
Result: In vivo pharmacokinetic indexes were t1/2 (0.5 h), C0 (37 ng/mL), AUC0-∞ (18 h*ng/mL), CLobs (54 L/h/kg), and Vss,obs (32 L/kg), respectively.
分子量

358.44

Formula

C22H22N4O

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献

CSF1R-IN-15 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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.

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产品名称:
CSF1R-IN-15
目录号:
HY-155001
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