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Submit ReviewPexidartinib is a potent colony-stimulating factor-1 receptor (CSF-1R) tyrosine kinase inhibitor (IC50 = 20 nM). In the B16F10 mouse melanoma model, Pexidartinib reduces the systemic and local accumulation of macrophages without affecting Gr-1+ myeloid derived suppressor cells. When combined with tumor-specific CD8 T cell immunotherapy, Pexidartinib promotes the control of tumor growth. In the BRAFV600E-driven mouse melanoma model, Pexidartinib improves the efficacy of adoptive cell therapy with reduction of TIMs and an increase in tumor-infiltrating lymphocytes and T cells. Orally bioavailable.
Pexidartinib is also offered as part of the Tocriscreen Kinase Inhibitor Library. 了解 Tocris 化合物库的更多信息。
分子量 | 417.82 |
公式 | C20H15ClF3N5 |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 1029044-16-3 |
PubChem ID | 25151352 |
InChI Key | JGWRKYUXBBNENE-UHFFFAOYSA-N |
Smiles | ClC1=CC2=C(N=C1)NC=C2CC(C=C3)=CN=C3NCC(C=C4)=CN=C4C(F)(F)F |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 41.78 | 100 |
以下数据基于产品分子量 417.82。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2.39 mL | 11.97 mL | 23.93 mL |
5 mM | 0.48 mL | 2.39 mL | 4.79 mL |
10 mM | 0.24 mL | 1.2 mL | 2.39 mL |
50 mM | 0.05 mL | 0.24 mL | 0.48 mL |
参考文献是支持产品生物活性的出版物。
DeNardo et al (2011) Leukocyte complexity predicts breast cancer survival and functionally regulates response to chemotherapy. Cancer Discov. 1 54 PMID: 22039576
Mok et al (2014) Inhibition of CSF-1 receptor improves the antitumor efficacy of adoptive cell transfer immunotherapy. Cancer Res. 74 153 PMID: 24247719
Sluijter et al (2014) Inhibition of CSF-1R supports T-cell mediated melanoma therapy. PLoS One. 9 e104230 PMID: 25110953
If you know of a relevant reference for Pexidartinib, please let us know.
关键词: Pexidartinib, Pexidartinib supplier, potent, receptor, tyrosine, kinases, inhibitors, inhibits, colony-stimulating, factor-1, CSF-1R, CSF1R, Other, RTKs, 7590, Tocris Bioscience
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