Testing Data
MK-2206, inhibitor
MK-2206
Purity
0.99
Synonyms
MK-2206; inhibitor
Purity/Purification
0.99
Solubility
DMSO >=96mg/mL - Water >=96mg/mL - Ethanol >=2mg/mL
Formula
C25H21N5O.2HCl
CAS Number
1032350-13-2
Preparation and Storage
Store at-20 degree C 2 years.
Testing Data
Testing Data
Related Product Information for MK-2206, inhibitor
MK-2206 dihydrochloride is a highly selective, potent non-ATP competitive allosteric Akt inhibitor with IC50 of 5.3 nM, 12 nM, 65 nM for Akt1, Akt2 and Akt3 respectively. MK-2206 dihydrochloride possesses extensively preclinical antitumor activity. In vitro, MK-2206 dihydrochloride synergistically inhibited cell proliferation of human cancer cell lines in combination with molecular targeted agents such as erlotinib or lapatinib. Complementary prevention of erlotinib-insensitive Akt phosphorylation by MK-2206 dihydrochloride was one mechanism of synergism, and a synergistic effect was found even in erlotinib-insensitive cell lines. 1 hr treatment of 1 muM MK-2206 abolished Akt phosphorylation in U87MG cells. MK-2206 dihydrochloride treatment abolished IR-induced Akt phosphorylation. Moreover, treatment with MK-2206 also increased the radiosensitivity of U87MG cells. [1] MK-2206 dihydrochloride also revealed synergistic responses in combination with cytotoxic agents such as topoisomerase inhibitors (doxorubicin, camptothecin), antimetabolites (gemcitabine, 5-fluorouracil), anti-microtubule agents (docetaxel), and DNA cross-linkers (carboplatin) in lung NCI-H460 or ovarian A2780 tumor cells. The synergy with docetaxel depended on the treatment sequence; a schedule of MK-2206 dosed before docetaxel was not effective. MK-2206 inhibited the Akt phosphorylation that is induced by carboplatin and gemcitabine. [1] In vivo, MK-2206 dihydrochloride in combination with these agents exerted significantly more potent tumor inhibitory activities than each agent in the monotherapy setting. MK-2206 dihydrochloride is generally well tolerated at doses up to 60 mg QOD with plasma concentrations that portend activity in preclinical models. PK/PD results suggest a substantial and maintained target inhibition should at 60 mg. [2] The phase II clinical trials of MK-2206 dihydrochloride against the treatment of endometrial cancer are recruiting participant Dana-Farber Cancer Institute.
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Product Notes
The MK-2206 (Catalog #AAA8506259) is an Inhibitor and is intended for research purposes only. The product is available for immediate purchase. It is sometimes possible for the material contained within the vial of "MK-2206, Inhibitor" to become dispersed throughout the inside of the vial, particularly around the seal of said vial, during shipment and storage. We always suggest centrifuging these vials to consolidate all of the liquid away from the lid and to the bottom of the vial prior to opening. Please be advised that certain products may require dry ice for shipping and that, if this is the case, an additional dry ice fee may also be required.Precautions
All products in the AAA Biotech catalog are strictly for research-use only, and are absolutely not suitable for use in any sort of medical, therapeutic, prophylactic, in-vivo, or diagnostic capacity. By purchasing a product from AAA Biotech, you are explicitly certifying that said products will be properly tested and used in line with industry standard. AAA Biotech and its authorized distribution partners reserve the right to refuse to fulfill any order if we have any indication that a purchaser may be intending to use a product outside of our accepted criteria.Disclaimer
Though we do strive to guarantee the information represented in this datasheet, AAA Biotech cannot be held responsible for any oversights or imprecisions. AAA Biotech reserves the right to adjust any aspect of this datasheet at any time and without notice. It is the responsibility of the customer to inform AAA Biotech of any product performance issues observed or experienced within 30 days of receipt of said product. To see additional details on this or any of our other policies, please see our Terms & Conditions page.Item has been added to Shopping Cart
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