Pexidartinib

Pricing Availability   Qty
说明: Potent CSF-1R inhibitor
化学名: N-[5-[(5-Chloro-1H-pyrrolo[2,3-b]pyridin-3-yl)methyl]-2-pyridinyl]-6-(trifluoromethyl)-3-pyridinemethanamine
纯度: ≥98% (HPLC)
说明书
引用文献
评论

生物活性 for Pexidartinib

Pexidartinib 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.

化合物库 for Pexidartinib

Pexidartinib is also offered as part of the Tocriscreen Kinase Inhibitor Library. 了解 Tocris 化合物库的更多信息。

技术数据 for Pexidartinib

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.

溶解性数据 for Pexidartinib

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 41.78 100

制备储备液 for Pexidartinib

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.

选择批次从而根据批次分子量重新计算:
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

Molarity Calculator

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Reconstitution Calculator

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Dilution Calculator

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参考文献 for Pexidartinib

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


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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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