- GSK1904529A
- BMS-536924
- Linsitinib
- NVP-AEW541
- BMS-754807
- AXL1717
| AG-1024Selective IGF-1R inhibitor |
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 = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
| Description | AG-1024 isa selective inhibitor of IGF-1R with IC50 value of 7 μM. | |||||
| Targets | IGF-1R | |||||
| IC50 | 7 μM | |||||
| Cell experiment: [1] | |
Cell lines | MCF-7 |
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 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months. |
Reaction Conditions | 10 nM, 5 days for cell proliferation inhibition 10 nM, 48 hours for apoptosis induction |
Applications | The Tyrphostin AG-1024 induced a marked decrease of cell proliferation in a time-dependent manner. It also potently induced cell apoptosis with a 20.1 % of apoptotic cells. |
| Animal experiment : [2] | |
Animal models | Female nude mice implanted with Ba/F3-p210 cells |
Dosage form | Intraperitoneal injection, 30 μg in100 μl, once per day for 10 days |
Applications | After injection with Ba/F3-p210 cells (Bcr-Abl expressing cells), nude mice were injected after 6 days with PBS 0.1 ml (control) or Tyrphostin AG1024 30 μg/100 μl (1 μl of 980 μM). The growth of the Ba/F3-p210 xenografts was significantly delayed when mice were treated with Tyrphostin AG1024. |
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] Wen B, Deutsch E, Marangoni E, et al. Tyrphostin AG 1024 modulates radiosensitivity in human breast cancer cells. British journal of cancer, 2001, 85(12): 2017. [2] Deutsch E, Maggiorella L, Wen B, et al. Tyrosine kinase inhibitor AG1024 exerts antileukaemic effects on STI571-resistant Bcr-Abl expressing cells and decreases AKT phosphorylation. British journal of cancer, 2004, 91(9): 1735-1741. | |
AG-1024 Dilution Calculator
calculate
AG-1024 Molarity Calculator
calculate
| Cas No. | 65678-07-1 | SDF | Download SDF |
| Chemical Name | 2-[(3-bromo-5-tert-butyl-4-hydroxyphenyl)methylidene]propanedinitrile | ||
| Canonical SMILES | CC(C)(C)C1=C(C(=CC(=C1)C=C(C#N)C#N)Br)O | ||
| Formula | C14H13BrN2O | M.Wt | 305.17 |
| Solubility | ≥15.25mg/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. | ||
AG1024 is an inhibitor of insulin-like growth factor-1 receptor (IGF-1R) and insulin receptor (IR) that specifically inhibits autophosphorylation of IGF-1R and IR with IC50 values of 7μM and 57 μm, respectively [1].
AG1024 has shown to inhibit IGF-1- and insulin-stimulated cellular proliferation in NIH-3T3 mouse fibroblast cells with IC50 values of 0.4μM and 0.1μM, respectively. Additionally, AG1024 shows to block tyrosine kinase activity towards exogenous substrates (TKA) with IC50 values of 18μM and 80μM [1].
AG1024 has been reported to block receptor tyrosine kinase activity, resulting in abolishment of MAPK and Akt pathways and inhibition of cell growth. Moreover, studies showed that AG1024 concentration-dependently inhibited E2 stimulation in MCF-7:PF cells [2].
References:[1] Párrizas M1, Gazit A, Levitzki A, Wertheimer E, LeRoith D. Specific inhibition of insulin-like growth factor-1 and insulin receptor tyrosine kinase activity and biological function by tyrphostins. Endocrinology. 1997 Apr;138(4):1427-33.[2] Fan P1, Agboke FA1, McDaniel RE1, Sweeney EE1, Zou X1, Creswell K1, Jordan VC2.Inhibition of c-Src blocks oestrogen-induced apoptosis and restores oestrogen-stimulated growth in long-term oestrogen-deprived breast cancer cells. Eur J Cancer. 2014 Jan; 50(2):457-68.
