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Submit Review1A-116 is a Rac1 inhibitor. Reduces intracellular Rac1-GTP levels and blocks Rac1-P-Rex1 interaction in vitro. Exhibits no effect on GTPase activity of closely related Cdc42. Displays antiproliferative, anti-invasive and pro-apoptotic activity in several cancer cell lines. Exhibits antimetastatic activity in vivo. Also restores antiproliferative effects of Tamoxifen (Cat. No. 6342) in resistant breast cancer cell.
Sold under license from Romikin S.A.
1A-116 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
分子量 | 307.31 |
公式 | C16H16F3N3 |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 1430208-73-3 |
PubChem ID | 71543346 |
InChI Key | DVIJFJSZZNOTLP-UHFFFAOYSA-N |
Smiles | CC1=CC(NC(NC2=C(C(F)(F)F)C=CC=C2)=N)=CC(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 | 30.73 | 100 | |
ethanol | 30.73 | 100 |
以下数据基于产品分子量 307.31。 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 | 3.25 mL | 16.27 mL | 32.54 mL |
5 mM | 0.65 mL | 3.25 mL | 6.51 mL |
10 mM | 0.33 mL | 1.63 mL | 3.25 mL |
50 mM | 0.07 mL | 0.33 mL | 0.65 mL |
参考文献是支持产品生物活性的出版物。
Cardama et al (2014) Preclinical development of novel Rac1-GEF signaling inhibitors using a rational design approach in highly aggressive breast cancer cell lines. Anticancer Agents Med.Chem. 14 840 PMID: 24066799
Gonzalez et al (2017) Pharmacological inhibition of Rac1-PAK1 axis restores tamoxifen sensitivity in human resistant breast cancer cells. Cell Signal. 30 154 PMID: 27939839
Cabrera et al (2017) Pharmacological Rac1 inhibitors with selective apoptotic activity in human acute leukemic cell lines. Oncotarget. 8 98509 PMID: 29228706
If you know of a relevant reference for 1A-116, please let us know.
关键词: 1A-116, 1A-116 supplier, rac1, gtpase, inhibitors, inhibits, tamoxifen, resistance, breast, cancer, Rho, 6701, Tocris Bioscience
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