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Submit ReviewPND 1186 is a potent FAK inhibitor (IC50 values are 1.5 and 100 nM for recombinant FAK and FAK in breast carcinoma cells, respectively). Promotes caspase activation; triggering apoptosis. Inhibits 4T1 breast carcinoma subcutaneous tumor growth and breast carcinoma cell motility. Decreases spontaneous breast to lung metastasis in pre-clinical models. Orally bioavailable.
PND 1186 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 | 501.51 |
公式 | C25H26F3N5O3 |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 1061353-68-1 |
PubChem ID | 25073775 |
InChI Key | IGUBBWJDMLCRIK-UHFFFAOYSA-N |
Smiles | CNC(=O)C1=C(NC2=CC(NC3=C(OC)C=C(C=C3)N3CCOCC3)=NC=C2C(F)(F)F)C=CC=C1 |
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 | 50.15 | 100 |
以下数据基于产品分子量 501.51。 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 | 1.99 mL | 9.97 mL | 19.94 mL |
5 mM | 0.4 mL | 1.99 mL | 3.99 mL |
10 mM | 0.2 mL | 1 mL | 1.99 mL |
50 mM | 0.04 mL | 0.2 mL | 0.4 mL |
参考文献是支持产品生物活性的出版物。
Walsh et al (2010) Oral delivery of PND-1186 FAK inhibitor decreases tumor growth and spontaneous breast to lung metastasis in pre-clinical models. Cancer Biol.Ther. 9 778 PMID: 20234193
Tanjoni et al (2010) PND-1186 FAK inhibitor selectively promotes tumor cell apoptosis in three-dimensional environments. Cancer Biol.Ther. 9 764 PMID: 20234191
Jiang et al (2016) Targeting focal adhesion kinase renders pancreatic cancers responsive to checkpoint immunotherapy. Nat.Med. 22 851 PMID: 27376576
If you know of a relevant reference for PND 1186, please let us know.
关键词: PND 1186, PND 1186 supplier, PND1186, SR2516, VS4718, SR_2516, VS_4718, potent, FAK, inhibitors, inhibits, orally, bioavailable, caspase, activators, Focal, Adhesion, Kinase, 6891, Tocris Bioscience
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