GSK690693

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AdipoGen Life Sciences
Product Code: AG-CR1-3628
CodeSizePrice
AG-CR1-3628-M0055 mg£100.00
Quantity:
AG-CR1-3628-M02525 mg£350.00
Quantity:
Prices exclude any Taxes / VAT

Overview

Antibody Isotype: n/a
Antibody Clone: n/a
Regulatory Status: RUO
Shipping:
-20°C
Storage:
-20°C

Images

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Chemical Structure
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Chemical Structure

Documents

Further Information

Alternate Names/Synonyms:
GSK-690693
Appearance:
Off-white to pale yellow solid.
CAS:
937174-76-0
Class:
6.1
EClass:
32160000
Form (Short):
liquid
GHS Symbol:
GHS06
Hazards:
H301
InChi:
InChI=1S/C21H27N7O3/c1-4-28-18-15(30-12-13-6-5-9-23-10-13)11-24-14(7-8-21(2,3)29)16(18)25-20(28)17-19(22)27-31-26-17/h11,13,23,29H,4-6,9-10,12H2,1-3H3,(H2,22,27)/t13-/m0/s1
InChiKey:
KGPGFQWBCSZGEL-ZDUSSCGKSA-N
Long Description:
Chemical. CAS: 937174-76-0. Formula: C21H27N7O3. MW: 425.5. pan-Akt inhibitor targeting Akt1, 2, 3 with IC50 values of 2, 13 and 9 nM, respectively. Inhibits AMPK, DAPK3, PAK4, 5 and 6, as well as members of the AGC kinase family including PKA, PrkX and PKC isoforms (IC50 < 100 nM). Occupies the ATP binding pocket of the kinase domain and competes with ATP. Anti-cancer compound both in vitro and in vivo. Blocks the phosphorylation of downstream targets of ATK in a dose-dependent manner, which leads to antiproliferative and apoptotic effects in tumor cell lines. Induces hyperglycemia related to peripheral insulin resistance, increased gluconeogenesis, and/or hepatic glycogenolysis.
MDL:
MFCD14105605
Molecular Formula:
C21H27N7O3
Molecular Weight:
425.5
Package Type:
Vial
PG:
III
Precautions:
P264, P301, P310, P330
Product Description:
pan-Akt inhibitor targeting Akt1, 2, 3 with IC50 values of 2, 13 and 9 nM, respectively. Inhibits AMPK, DAPK3, PAK4, 5 and 6, as well as members of the AGC kinase family including PKA, PrkX and PKC isoforms (IC50 < 100 nM). Occupies the ATP binding pocket of the kinase domain and competes with ATP. Anti-cancer compound both in vitro and in vivo. Blocks the phosphorylation of downstream targets of ATK in a dose-dependent manner, which leads to antiproliferative and apoptotic effects in tumor cell lines. Induces hyperglycemia related to peripheral insulin resistance, increased gluconeogenesis, and/or hepatic glycogenolysis.
Purity:
>95%
Signal word:
Danger
SMILES:
[H][C@]1(COC2=C3N(CC)C(=NC3=C(N=C2)C#CC(C)(C)O)C2=NON=C2N)CCCNC1
Solubility Chemicals:
Soluble in DMSO. Slightly soluble in ethanol (<1mg/ml).
Transportation:
Excepted Quantity
UN Nummer:
UN 2811
UNSPSC Category:
Biochemical Reagents
UNSPSC Number:
12352200
Use & Stability:
Stable for at least 2 years after receipt when stored at -20°C.

References

Identification of 4-(2-(4-amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-{[(3S)-3-piperidinylmethyl]oxy}-1H-imidazo[4,5-c]pyridin-4-yl)-2-methyl-3-butyn-2-ol (GSK690693), a novel inhibitor of AKT kinase: D.A. Heerding, et al.; J. Med. Chem. 51, 5663 (2008) | Characterization of an Akt kinase inhibitor with potent pharmacodynamic and antitumor activity: N. Rhodes, et al.; Cancer Res. 68, 2366 (2008) | AKT inhibitor, GSK690693, induces growth inhibition and apoptosis in acute lymphoblastic leukemia cell lines: D.S. Levy, et al.; Blood 113, 1723 (2009) | Mechanism and management of AKT inhibitor-induced hyperglycemia: M.C. Crouthamel, et al.; Clin. Cancer Res. 15, 217 (2009) | GSK690693 delays tumor onset and progression in genetically defined mouse models expressing activated Akt: D.A. Altomare, et al.; Clin. Cancer Res. 16, 486 (2010) | Akt inhibitors in clinical development for the treatment of cancer: S.K. Pal, et al.; Expert Opin. Investig. Drugs 19, 1355 (2010) | Characterization of a chemical affinity probe targeting Akt kinases: F. Pachl, et al.; J. Proteome Res. 12, 3792 (2013)

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