GSK-690693
This product is for research use only, not for human use. We do not sell to patients.
For small sizes, please check our retail website as below: www.invivochem.com
| Size | Price | Stock |
|---|---|---|
| 250mg | $1450 | Check With Us |
| 500mg | $2400 | Check With Us |
| 1g | $3600 | Check With Us |
: Cat #: V0157 CAS #: 937174-76-0 Purity ≥ 98%
Description: GSK690693, an aminofurazan derivative, is a novel, potent and ATP-competitive pan-Akt inhibitor targeting Akt1/2/3 with potential anticancer activity.
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| Molecular Weight (MW) | 425.48 |
|---|---|
| Molecular Formula | C21H27N7O3 |
| CAS No. | 937174-76-0 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in sol | |
| Solubility In Vitro | DMSO: 39 mg/mL (91.7 mM)r |
| Water: <1 mg/mLr | |
| Ethanol: <1 mg/mL | |
| Solubility In Vivo | 15% Captisol: 30 mg/m |
| SMILES Code | CC(O)(C)C#CC1=NC=C(OC[C@@H]2CNCCC2)C3=C1N=C(C4=NON=C4N)N3CC |
| Synonyms | GSK690693; GSK-690693; GSK 690693 |
| Protocol | In Vitro | GSK690693 is very selective for the Akt isoforms versus the majority of kinases in other families. However, GSK690693 is less selective for members of the AGC kinase family including PKA, PrkX, and PKC isozymes with IC50 of 24 nM, 5 nM, and 2-21 nM, respectively. GSK690693 also potently inhibits AMPK and DAPK3 from the CAMK family with IC50 of 50 nM and 81 nM, respectively, and PAK4, 5, and 6 from the STE family with IC50 of 10 nM, 52 nM, and 6 nM, respectively. GSK690693 inhibits the phosphorylation of GSK3β in tumor cells with IC50 ranging from 43 nM to 150 nM. GSK690693 treatment leads to a dose-dependent increase in the nuclear accumulation of the transcription factor FOXO3A. GSK690693 potently inhibits the proliferation of T47D, ZR-75-1, BT474, HCC1954, MDA-MB-453, and LNCaP cells with IC50 of 72 nM, 79 nM, 86 nM, 119 nM, 975 nM, and 147 nM, respectively. GSK690693 treatment induces apoptosis at concentrations > 100 nM in both LNCaP and BT474 cells. |
|---|---|---|
| In Vivo | A single administration of GSK690693 inhibits GSK3β phosphorylation in human breast carcinoma (BT474) xenografts in a dose- and time-dependent manner. Similarly, GSK690693 induces a reduction in phosphorylation of the Akt substrates, PRAS40, and FKHR/FKHRL1. GSK690693 also results in an acute increase in blood glucose, returning to baseline 8 to 10 hours after drug administration. Administration of GSK690693 induces reductions in phosphorylated Akt substrates in vivo, and potently inhibits the growth of human SKOV-3 ovarian, LNCaP prostate, and BT474 and HCC-1954 breast carcinoma xenografts, with maximal inhibition of 58% to 75% at the dose of 30 mg/kg/day. |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 2.3503 mL | 11.7514 mL | 23.5029 mL | 47.0057 mL |
| 5mM | 0.4701 mL | 2.3503 mL | 4.7006 mL | 9.4011 mL |
| 10mM | 0.2350 mL | 1.1751 mL | 2.3503 mL | 4.7006 mL |
| 20mM | 0.1175 mL | 0.5876 mL | 1.1751 mL | 2.3503 mL |
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Method for preparing in vivo formulation:
Take
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PEG300, mix and clarify, next add
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Tween 80,mix and clarify, next add
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ddH2O,mix and clarify.
Note:
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