Pexidartinib (PLX3397)
![mRNA synthesis](/media/diy/images/page/figure1-mrna.png)
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
![Tyramine Signal Amplification (TSA)](/media/diy/images/page/figure2-01.png)
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
![screening library](/media/diy/images/page/figure3-01.png)
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
![Cell Counting Kit-8 (CCK-8)](/media/diy/images/page/CCK-8.jpg)
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
![SYBR Safe DNA Gel Stain](/media/diy/images/page/SYBR Safe DNA Gel Stain.png)
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
![Inhibitor Cocktails](/media/diy/images/page/Inhibitor Cocktails.jpg)
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
集落刺激因子1(CSF1)是参与组织巨噬细胞招募和活化的关键细胞因子,通过结合高亲和力的受体酪氨酸激酶CFMS/CSF1受体发挥以上效应.Pexidartinib (PLX3397)是CSF-1R的抑制剂,可以穿越血脑屏障.
体外实验:PLX3397强烈衰减由B16F10黑色素瘤驱动的巨噬细胞的全身和局部积累,不影响Gr-1+骨髓衍生的抑制性细胞[1].
在体实验:野生型的C57小鼠原位注射GL261细胞,使用PLX3397化合物口服2周后,对照组的肿瘤显示广泛的小胶质细胞浸润.在PLX3397处理的动物中,肿瘤中Iba1-阳性细胞的数量显著减少[2].
临床试验:在Ib期试验中,晚期实体瘤患者每周使用紫杉醇和口服不断升级剂量的PLX3397,建立PLX3397的RP2D.这项研究将支持I-SPY-2新辅助化疗的乳腺癌实验中PLX3397-紫杉醇组合治疗的进一步发展.
参考文献:
[1] Sluijter M, van der Sluis TC, van der Velden PA, Versluis M, West BL, van der Burg SH, van Hall T. Inhibition of CSF-1R supports T-cell mediated melanoma therapy. PLoS One. 2014 Aug 11;9(8):e104230.
[2] Coniglio SJ, Eugenin E, Dobrenis K, Stanley ER, West BL, Symons MH, Segall JE. Microglial stimulation of glioblastoma invasion involves epidermal growth factor receptor (EGFR) and colony stimulating factor 1 receptor (CSF-1R) signaling. Mol Med. 2012 May 9;18:519-27.
- 1. Jinchao Gao, Qingxiang Song, et al. "Intracerebral fate of organic and inorganic nanoparticles is dependent on microglial extracellular vesicle function." Nat Nanotechnol. 2024 Mar;19(3):376-386. PMID: 38158436
- 2. Sanghoon Lee, Rebekah Karns, et al. "Mechanism of paracrine communications between hepatic progenitor cells and endothelial cells." Cell Signal. 2022 Aug 30;100:110458. PMID: 36055565
- 3. Nina M. Dräger, Sydney M. Sattler, et al. "A CRISPRi/a platform in human iPSC-derived microglia uncovers regulators of disease states." Nat Neurosci. 2022 Sep;25(9):1149-1162. PMID: 35953545
- 4. Komohara Y, Noyori O, et al. "Potential anti-lymphoma effect of M-CSFR inhibitor in adult T-cell leukemia/lymphoma." J Clin Exp Hematop. 2018;58(4):152-160. PMID: 30541986
- 5. Yu R, Jin H, et al. "Inhibition of the CSF-1 receptor sensitizes ovarian cancer cells to cisplatin." Cell Biochem Funct. 2018 Jan 25. PMID: 29372560
- 6. Wang C, Yeo S, et al. "Autophagy gene FIP200 in neural progenitors non-cell autonomously controls differentiation by regulating microglia." J Cell Biol. 2017 Jun 20. pii: jcb.201609093. PMID: 28634261
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 417.81 |
Cas No. | 1029044-16-3 |
Formula | C20H15ClF3N5 |
Solubility | insoluble in EtOH; insoluble in H2O; ≥20.9 mg/mL in DMSO |
Chemical Name | 5-((5-chloro-1H-pyrrolo[2,3-b]pyridin-3-yl)methyl)-N-((6-(trifluoromethyl)pyridin-3-yl)methyl)pyridin-2-amine |
SDF | Download SDF |
Canonical SMILES | ClC(C=N1)=CC2=C1NC=C2CC3=CN=C(NCC4=CN=C(C(F)(F)F)C=C4)C=C3 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
细胞实验 [1]: | |
细胞系 |
SK-N-SH细胞 |
溶解方法 |
该化合物在DMSO中的溶解度大于20.9 mg/mL。若获取更高浓度的溶液,可在37℃下孵育10分钟,随后在超声波浴中摇匀。-20℃以下可储存数月。 |
反应条件 |
IC50: 10 μM |
应用 |
Pexidartinib微弱抑制SK-N-SH细胞的生长,IC50为10 μM。PLX3397对MDA-MB-231人肿瘤细胞异种移植物的生长几乎没有影响。 |
动物实验 [1,2]: | |
动物模型 |
B16F10黑色素瘤细胞异种移植的C57BL/6小鼠,携带MDA-MB-468人乳腺肿瘤细胞异种移植物的雌性裸鼠。 |
给药剂量 |
口服,每日剂量约45 mg/kg |
应用 |
Pexidartinib主要影响F4/80+ Ly6C-血液巨噬细胞,并且强烈降低F4/80+Ly6C+'炎性'单核细胞的CSF-1R表达水平。口服给药PLX3397可以防止破骨细胞的增加和骨骼的损失。 |
注意事项 |
由于实验环境的不同,实际溶解度可能与理论值略有不同,请测试室内所有化合物的溶解度。 |
References: [1] West B L, DeNardo D G, Tsai J, et al. Efficacy of the selective CSF-1R kinase inhibitor PLX3397 in mouse models of tumor growth and bone metastasis[J]. 2010. [2] Sluijter M, van der Sluis T C, van der Velden P A, et al. Inhibition of CSF-1R supports T-cell mediated melanoma therapy[J]. PloS one, 2014, 9(8): e104230. |
质量控制和MSDS
- 批次:
化学结构
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