- AT7867
- AT7867 dihydrochloride
- 1-Azakenpaullone
- H 89 2HCl
- Dinaciclib (SCH727965)
- PHA-793887
| A-674563Akt1/PKA/CDK2 inhibitor,potent and selective |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
Nature.2018 Nov;563(7731):407-411.Nature.2018 Jun 13.Nature.2018 Jun 27.Nature.2018 Mar 29;555(7698):673-677.Nature.2017 Sep 7;549(7670):96-100.Nature.2016 Apr 21;532(7599):398-401.
Science.2016 Aug 5;353(6299)594-8Nat Nanotechnol.2017 Dec;12(12):1190-1198.Nature Biotechnology.2017 Jun;35(6):569-576Nat Med.2018 Sep 17.Cell.2018 Dec 21. pii: S0092-8674(18)31561-7.Cell.Available online 25 October 2018.Cell.2018 Sep 27. pii: S0092-8674(18)31183-8.Cell.2018 Jun 28;174(1):172-186.e21.Cell.2018 Feb 22;172(5):1007-1021.e17.Cell.2017 Nov 30;171(6):1284-1300.e21.Cell.2017 Aug 17. pii: S0092-8674(17)30869-3.Cell.2017 Jul 13;170(2):312-323Nat Med.2018 Jan 29.Nat Med.2017 Nov;23(11):1342-1351.Cell.2017 Apr 6;169(2):286-300.Cell.2015 Aug 27;162(5):987-1002.Cell.2015 Feb 12;160(4):729-44.Nature Medicine.2017 Apr;23(4):493-500.Cancer Cell.2018 May 14;33(5):905-921.e5.Cancer Cell.2018 Apr 9;33(4):752-769.e8.Cancer Cell.2018 Mar 12;33(3):401-416.e8.Cancer Cell.2017 Aug 14;32(2):253-267.e5.Nat Methods.2018 Jul;15(7):523-526.Cell Stem Cell.2018 May 3;22(5):769-778.e4.Cell Stem Cell.2017 Nov 20. pii: S1934-5909(17)30375-2.Quality Control & MSDS
- View current batch:
- Purity = 99.21%
- COA (Certificate Of Analysis)
- HPLC
- NMR (Nuclear Magnetic Resonance)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
| Description | A-674563 is an inhibitor of Akt1 with a Ki value of 11 nM. | |||||
| Targets | Akt1 | PKA | CDK2 | GSK-3β | ERK2 | |
| IC50 | 11 nM(Ki) | 16 nM(Ki) | 46 nM(Ki) | 110 nM(Ki) | 260 nM(Ki) | |
| Cell experiment [1]: | |
Cell lines | soft tissue sarcoma (STS) cell lines |
Preparation method | The solubility of this compound in DMSO is > 10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
Reacting condition | 0-10 μM; 24, 48, and 72 h |
Applications | In STS cell lines, A-674563 significantly decreased GSK3 and MDM2 phosphorylation in a dose-dependent way. A-674563 induced growth inhibition in a dose-dependent and time-dependent manner, and induced G2 cell cycle arrest and apoptosis. |
| Animal experiment [1]: | |
Animal models | Mice with human fibrosarcoma (HT1080) subcutaneous xenografts |
Dosage form | 20 mg/kg/bid, p.o. |
Application | In mice with human fibrosarcoma (HT1080) subcutaneous xenografts, A-674563 inhibited tumor growth and significantly reduced tumor volume at the termination of the study (320.76 ± 86.8) compared with that in control group (667.92 ± 97.41; P <> |
Other notes | Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
References: [1] Zhu QS, Ren W, Korchin B et al. Soft tissue sarcoma cells are highly sensitive to AKT blockade: a role for p53-independent up-regulation of GADD45 alpha. Cancer Res. 2008 Apr 15;68(8):2895-903. | |
A-674563 Dilution Calculator
calculate
A-674563 Molarity Calculator
calculate
| Cas No. | 552325-73-2 | SDF | Download SDF |
| Chemical Name | (2S)-1-[5-(3-methyl-2H-indazol-5-yl)pyridin-3-yl]oxy-3-phenylpropan-2-amine | ||
| Canonical SMILES | CC1=C2C=C(C=CC2=NN1)C3=CC(=CN=C3)OCC(CC4=CC=CC=C4)N | ||
| Formula | C22H22N4O | M.Wt | 358.44 |
| Solubility | ≥4.9mg/mL in DMSO | Storage | Store at -20°C |
| Physical Appearance | A solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
A-674563 is a potent and selective Akt1 inhibitor with IC50 value of 14 nM. A-67453 also inhibited PKA and Cdk2 with IC50 value of 16 nM and 46 nM.
Akt, also known as protein kinase B, is a serine/threonine-specific protein kinase that plays a key role in multiple cellular processes such as glucose metabolism, apoptosis, cell proliferation, transcription and cell migration.
In MiaPaCa-2 cells treated with A-674563 for 48 hour, it slowed the tumor cell proliferation (EC50 = 0.4 μm). In STS cells, phosphorylation of GSK3 and MDM2 was prominently reduced by A-674563 treatment. [1] Akt inhibition-induced G2 cells cycle arrest and apoptosis were also observed in A563-treated STS cells. [2]
In scid mice carrying established PC-3 tumors, administration of A-674563 at 40 mg/kg per day for 21 days, combined with administration of paclitaxel at 15 mg/kg per day on days 20.24.28, increased the efficacy of paclitaxel compared with paclitaxel monotherapy. [1] A563 also significantly blocked HT1080 xenograft growth in nude mice. [2]
References:1. Luo Y, Shoemaker AR, Liu X et al. Potent and selective inhibitors of Akt kinases slow the progress of tumors in vivo. Mol Cancer Ther. 2005 Jun;4(6):977-86.2. Zhu QS, Ren W, Korchin B et al. Soft tissue sarcoma cells are highly sensitive to AKT blockade: a role for p53-independent up-regulation of GADD45 alpha. Cancer Res. 2008 Apr 15;68(8):2895-903.
