Product Information

Biological Activity

MK-2206 dihydrochloride (MK-2206 (2HCl)) is an orally active allosteric AKT inhibitor with IC50s of 5 nM, 12 nM, and 65 nM for AKT1, AKT2, and AKT3, respectively[1].
MK-2206 dihydrochloride (MK-2206 (2HCl)) (0-10 ¦ÌM; 72 and 96 hours) inhibits the nasopharyngeal carcinoma (NPC) cell lines CNE-1, CNE-2, HONE-1, and SUNE-1 proliferation in dose- and time-dependent manner[1]. MK-2206 dihydrochloride (0-10 ¦ÌM; 24 and 48 hours) results in a dose-dependent increase in the percentage of cells in G0/G1 phase and a concomitant reduction of cell numbers in S phase in CNE-2 and HONE-1 cells[1]. MK-2206 dihydrochloride (0-10 ¦ÌM; 24 hours) attenuates phosphorylation levels of PRAS40 and S6 in a dose-dependent manner. MK-2206 does not effect phosphorylation of GSK¦Á/¦Â and AKT[1]. MK-2206 dihydrochloride (0-10 ¦ÌM; 24 hours) increases the appearance of LC3-II in CNE-2 cells dose-dependently. Microtubule-associated protein 1 LC3 is an essential autophagy protein[1].
Both MK-2206 dihydrochloride (MK-2206 (2HCl)) doses (oral gavage; 480 mg/kg once a week and 240 mg/kg three times a week; for 2 weeks) can inhibit the growth of human CNE-2 xenografts in nude mice. In the two MK-2206 dihydrochloride groups, the tumor weights are much lighter than the control group. Temporal body weight reduction is observed after receiving the MK-2206 dihydrochloride treatment[1]. No other obvious toxicity is observed in mice[1]. MK-2206 dihydrochloride (orally; 120 mg/kg; alternate days; for 3 weeks) significantly inhibits tumor growth[2].

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

Species

Mouse

Rat

Rabbit

Guinea pig

Hamster

Dog

Weight (kg)

0.02

0.15

1.8

0.4

0.08

10

Body Surface Area (m2)

0.007

0.025

0.15

0.05

0.02

0.5

Km factor

3

6

12

8

5

20

Animal A (mg/kg) = Animal B (mg/kg) multiplied by  (Animal B Km / Animal A Km)
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Order Information

Quantity

Price($)

Price($)

Availability

5mg

$115.00

€126.50

In stock

10mg

$165.00

€181.50

In stock

50mg

$385.00

€423.50

In stock

Free Delivery on orders over $350.00.

Chemical Information

Molecular Weight

480.39

Formula

C₂₅H₂₁N₅O.2HCl

CAS Number

1032350-13-2

Purity

>98.00%

Solubility

¡Ý 12.01mg/mL in DMSO

Storage

at -20¡ãC

Reference

[1]. Zhao YY, et al. Effects of an oral allosteric AKT inhibitor (MK-2206) on human nasopharyngeal cancer in vitro and in vivo. Drug Des Devel Ther. 2014 Oct 10;8:1827-37.
[2]. Agarwal E, et al. Akt inhibitor MK-2206 promotes anti-tumor activity and cell death by modulation of AIF and Ezrin in colorectal cancer. BMC Cancer. 2014 Mar 1;14:145.

We Devoted Ourselves To The Development Of Biomedical Research Reage

nt.