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Submit ReviewGNF 5 is a selective, non-ATP competitive allosteric inhibitor of Bcr-Abl (IC50 = 220 nM for wild-type Abl). Binds the myristate-binding site of Abl. Acts in combination with nilotinib to inhibit T315I Bcr-Abl in vitro and in vivo. Analog of GNF 2 (Cat. No. 4399). GNF 5 decreases mitochondrial function in lung cancer cells.
Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of GNF 5 is reviewed on the chemical probes website.
GNF 5 is also offered as part of the Tocriscreen Antiviral Library. 了解 Tocris 化合物库的更多信息。
分子量 | 418.37 |
公式 | C20H17F3N4O3 |
储存 | Store at +4°C |
纯度 | ≥98% (HPLC) |
CAS Number | 778277-15-9 |
PubChem ID | 44129660 |
InChI Key | IIQUYGWWHIHOCF-UHFFFAOYSA-N |
Smiles | O=C(NCCO)C1=CC(C2=NC=NC(NC3=CC=C(OC(F)(F)F)C=C3)=C2)=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 | 41.84 | 100 |
以下数据基于产品分子量 418.37。 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 | 11.95 mL | 23.9 mL |
5 mM | 0.48 mL | 2.39 mL | 4.78 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。
Zhang et al (2010) Targeting Bcr-Abl by combining allosteric with ATP-binding-site inhibitors. Nature 463 501 PMID: 20072125
Iacob et al (2011) Allosteric interactions between the myristate- and ATP-site of the Abl kinase. PLoS One 6 e15929 PMID: 21264348
Deng et al (2010) Expanding the diversity of allosteric Bcr-Abl inhibitors. J.Med.Chem. 53 6934 PMID: 20828158
Luttman et al (2021) ABL allosteric inhibitors synergize with statins to enhance apoptosis of metastatic lung cancer cells. Cell Rep. 37 109880 PMID: 34706244
If you know of a relevant reference for GNF 5, please let us know.
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