ABT-869 (Linifanib) is an aminobenzopyrazole-based, orally available, ATP-competitive receptor tyrosine kinase inhibitor with IC50 potency against KDR, FLT1, CSF-1R, FLT3, and PDGFRb of 4 nM, 3 nM, 3 nM, 4 nM, and 66 nM, respectively. It is highly selective (> 1uM) against unrelated tyrosine kinases and serine/threonine kinases. [1] In cellular assays, ABT-689 exhibited potency against ligand-induced PDGFRbeat, KIT, and CSF-1R phosphorylation, with IC50s of 2, 31, and 10 nM, respectively.In vivo, ABT-869 is orally effective in a wide range of human xenograft models, including MV4-11, HT1080, H526, DLD-1, A431, MX-1, MDA-231, MDA-435LM, and glioma 9L. [2] ABT-869 displays antiproliferative and apoptotic effects on cancer cells dependent on mutant kinases, such as FLT3. Consequently, ABT-869 is in clinical studies for the treatment of acute myeloid leukemia (AML). [3, 4] ABT-689 has been shown to induce apoptosis through an AKT and GSK-3beta-dependent pathway, thus suggesting that combination therapies with GSK-3beta inhibitors may be a promising approach to AML treatment. [3]
Technical information:
| Chemical Formula: | C21H18FN5O | |
| CAS #: | 796967-16-3 | |
| Molecular Weight: | 375.41 | |
| Purity: | > 98% | |
| Appearance: | White | |
| Chemical Name: | 1-(4-(3-amino-1H-indazol-4-yl)phenyl)-3-(2-fluoro-5-methylphenyl)urea | |
| Solubility: | Up to 100 mM in DMSO | |
| Synonyms: | ABT-869, ABT 869, ABT869, AL-39324, AL39324, Linifanib |
Shipping Condition: The product is shipped in a glass vial at ambient temperature.Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.
Reference:
| 1. | Albert et al., Preclinical activity of ABT-869, a multitargeted receptor tyrosine kinase inhibitor. Mol. Cancer Ther. 2006, 5, 995-1006. Pubmed ID:16648571 |
| 2. | Zhou et al., ABT-869, a promising multi-targeted tyrosine kinase inhibitor: from bench to bedside. J. Hematol. Oncol. 2009, 2, 33-45. Pubmed ID:19642998 |
| 3. | Hernandez-Davies et al., The multitargeted receptor tyrosine kinase inhibitor linifanib (ABT-869) induces apoptosis through an Akt and glycogen synthase kinase 3?-dependent pathway. Mol. Cancer Ther. 2011, 10, 949-959. Pubmed ID:21471285 |
| 4. | Shankar et al., ABT-869, a multitargeted receptor tyrosine kinase inhibitor: inhibition of FLT3 phosphorylation and signaling in acute myeloid leukemia. Blood, 2007, 109, 3400-3408. Pubmed ID:19642998 |
Other Information:
Product Specification (pdf) MSDS (pdf) Certificate of Analysis is available upon request.
ebiomall.com
>
>
>
>
>
>
>
>
>
>
>
支原体培养则是取样后在培养基上培养,看有多少支原体菌落会长出,是比较直观和可信的结果。
总体来讲,这两种检查手段可信度都较高,结合一起,不仅可以可靠的知道有无解脲支原体感染,还能知道感染是否严重。
RMgX + RX = R-R + MgX2.
这个反应需要的能量比生成格氏试剂的高,
因此降低反应温度是第一个选择。
其次, 增加镁得摩尔比, 让 RX与镁有更多机会反应, 而不是与RMgX。
第三, 降低RX的浓度, 即用更多的溶剂, 因为溶剂和格氏试剂有很显著的溶剂络合。
第四, 缓慢滴加RX., 即降低RX.在反应体系的浓度。
第五, 增加搅拌速率, 即, 让RX.与镁有更好的接触。
ajtr0009-1230.pdf(2384.3k)
该试剂盒是一种时间分辨的荧光共振能量转移免疫分析,该反应是一个竞争免疫反应,即铕标的cAMP示踪复合物与体系中的cAMP竞争结合标有Alexa Fluor 647染料的cAMP抗体。铕标cAMP示踪复合物是通过Biotin标记的cAMP与铕标的抗生物素蛋白链菌素(streptavidin)与抗体的复合物紧密结合产生的。
当抗体结合到示踪剂上时,340nm的激发光激发铕标分子,导致能量转移到Alexa Fluor 647染料上,结果产生665nm的发射光。荧光的强度与样品中的cAMP含量成反比。
本试剂盒用于检测在GPCR激动剂刺激下活细胞或者细胞膜制备品产生的cAMP。对于偶联Gαs的受体,激动剂刺激导致665nm的荧光强度降低,而拮抗剂则可以逆转这一效应;对于偶联Gαi的受体,在激动剂刺激的同时用forskolin刺激cAMP产生,那么激动剂则抑制forskolin诱导的cAMP的生成,因此对照只给forskolin的细胞组可以通过665nm荧光强度的增加反应激动剂的效应。
该试剂盒的灵敏度很高,室温下反应在20h内是稳定的。本试剂盒适用于在384孔板中进行24μl的微量分析。

