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Submit ReviewGNF 7 is a potent Bcr-Abl inhibitor (IC50 values are 61 and 133 nM for T315I and wild-type Bcr-Abl, respectively), inhibiting a range of clinically relevant Bcr-Abl mutants such as T315I, G250E, E255V, F317L and M351T. GNF 7 is also a Ras signaling inhibitor as well as inhibiting Ack1 and germinal center kinase (GCK). GNF 7 induces cell cycle arrest and apoptosis in leukemia cells harboring NRAS mutations, and shows growth inhibitory activity in human colon cancer cells. It prolongs survival in a leukemia cell xenotransplantation model in mice and is orally bioavailable.
分子量 | 547.53 |
公式 | C28H24F3N7O2 |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 839706-07-9 |
PubChem ID | 11478363 |
InChI Key | SZNYUUZOQHNEKB-UHFFFAOYSA-N |
Smiles | CC1=NC=C(NC2=NC=C(CN(C3=C(C)C=CC(NC(C4=CC(C(F)(F)F)=CC=C4)=O)=C3)C(N5C)=O)C5=N2)C=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 | 27.38 | 50 |
以下数据基于产品分子量 547.53。 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 |
---|---|---|---|
0.5 mM | 3.65 mL | 18.26 mL | 36.53 mL |
2.5 mM | 0.73 mL | 3.65 mL | 7.31 mL |
5 mM | 0.37 mL | 1.83 mL | 3.65 mL |
25 mM | 0.07 mL | 0.37 mL | 0.73 mL |
参考文献是支持产品生物活性的出版物。
Nonami et al (2015) Identification of novel therapeutic targets in acute leukemias with NRAS mutations using a pharmacologic approach. Blood 125 3133 PMID: 25833960
Choi et al (2010) A type-II kinase inhibitor capable of inhibiting the T315I "gatekeeper" mutant of Bcr-Abl. J.Med.Chem 53 5439 PMID: 20604564
If you know of a relevant reference for GNF 7, please let us know.
关键词: GNF 7, GNF 7 supplier, GNF7, RAS, inhibitors, inhibits, Ack1, germinal, centre, kinases, GCK, leukemia, TNK2, Bcr-Abl, GNF-7, Ras, GTPases, Abl, Kinase, 5607, Tocris Bioscience
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