Chemical Information:| Product Name | |
| Molecular Formula | C23H28N8OS |
| Molecular Weight | 464.59 |
| Storage | Store at -20°C |
| Targets | Aurora A | Aurora B | Aurora C |
| IC50 | 0.6 nM (Ki) | 4.6 nM (Ki) | 18 nM (Ki) |
| Dosage | 50 mg/kg, 75 mg/kg |
| Stability | 3 years - 20 ºC powder 6 months -80 ºC dissolved in a solvent |
| Solubility | Soluble in DMSO > 10 mM |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ºC and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20ºC for several months. |
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
Details:Synonyms:Cyclopropane carboxylic acid {4-[4-(4-methyl-piperazin-1-yl)-6-(5-methyl-2H-pyrazol-3-ylamino) -pyrimidin-2ylsulphanyl]-phenyl}-amide;VX-680/MK-0457;N-(4-(4-(5-methyl-1H-pyrazol-3-ylamino)-6-(1-methylpiperidin-4-ylamino)pyrimidin-2-ylthio)phenyl)cyclopropanecarboxamide;MK 0457;N-[4-[[4-(4-Methyl-1-piperazinyl)-6-[(5-methyl-1H-pyrazol-3-yl)amino]-2-pyrimidinyl]thio]phenyl]cyclopropanecarboxamide;Tozasertib;VX 680;Cyclopropanecarboxamide, N-(4-((4-(4-methyl-1-piperazinyl)-6-((5-methyl-1H-pyrazol-3-yl)amino)-2-pyrimidinyl)thio)phenyl)-
Description:VX-680 is an inhibitor of Aurora with Ki values of 0.6 nM, 4.6 nM, 18 nM, 30 nM and 30 nM for Aurora A, C, B, FLT3 and Bcr-Abl, respectively.
Application:While the VX-680 has a multi-kinase properties, VX-680 was induced cytotoxicity similar, IC50 of approximately 300 nM, in G2 / M phase, endoreduplication stage, and apoptosis ABL transfected BaF3 or FLT-3 kinase when, it displays a similar inhibition of Aurora B phenotype. VX-680 CAL-62 inhibition of cell proliferation, this effect time-dependent existence. Treatment with VX-680 14 days significantly reduced the number and size of population, treatment 8305C decline reached 70%, treatment CAL-62, 8505C, and BHT-101 fell 90%. VX-680 treated with different ATC cells, inhibition of cell proliferation, IC50 of 25 to 150 nM, this effect there is a time and dose dependent manner. In soft agar, VX-680 significantly undermine the ability of different cell lines formed communities. caspase-3 activity analysis display VX-680 induced apoptosis in different cell. VX-680 treatment CAL-62 cells 12 hours, the formation of DNA content ≥4N cell buildup. Micro-speed photographic analysis showed that CAL-62 VX-680-treated cells leave the cell medium term. VX-680 can inhibit the phosphorylation of histone H3. [2] VX-680 acts on the carrying T315I mutant BCR-Abl of patient samples, with a significant inhibitory activity. [3]
Notification:This compound is used only for research and not for human trials!
Other Small Molecular API:| AZD9291 | 1421373-65-0 |
| E7080 | 417716-92-8 |
| Afatinib diMaleate | 439081-18-2 |
| XL184 S-MALATE | 1140909-48-3 |
| Crizotinib | 877399-52-5 |
| Axitinib | 319460-85-0 |
| WZ4002 | 1213269-23-8 |
| Vandetanib | 443913-73-3 |
| Sunitinib | 557795-19-4 |
| Regorafenib | 755037-03-7 |
| Imatinib | 152459-95-5 |
| Foretinib | 849217-64-7 |
| trametinib | 871700-17-3 |
| Tivozanib | 475108-18-0 |
| Pelitinib | 257933-82-7 |
| Cediranib | 288383-20-0 |
| Selumetinib | 606143-52-6 |
| Tozasertib | 639089-54-6 |
| CapMatinib | 1029712-80-8 |
| Amuvatinib | 850879-09-3 |
| Lestaurtinib | 111358-88-4 |
| Brivanib | 649735-46-6 |
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Wuhan Biocar Bio-Pharm Co., Ltd was founded in 2001, formerly known as Tongshan Pharmaceutical Factory Company, which is a national high-tech enterprises. In 2014, in the process of creating a National Industrial Base, the Board of Directors decided to move the headquarter to Wuhan Biomedical Park. At the same time, with the advantages of the park policy, we carry out production and research cooperation with Humanwell Healthcare Gruop Co., Ltd, officially changed its name to Biocar Bio-Pharm Co., Ltd.
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