INY-03-041 trihydrochloride
Based on 1 publication(s) in Google Scholar
INY-03-041 trihydrochloride is a potent, highly selective and PROTAC-based pan-AKT degrader consisting of the ATP-competitive AKT inhibitor Ipatasertib (HY-15186) conjugated to Lenalidomide (HY-A0003). INY-03-041 trihydrochloride inhibits AKT1, AKT2 and AKT3 with IC50s of 2.0, 6.8 and 3.5 nM, respectively.
(Pink: Akt ligand (HY-130988); Blue: Cereblon ligand (HY-43722); Black: linker (HY-130985)).
For research use only. We do not sell to patients.
- Purity: 96.73%
- Formula: C44H59Cl4N7O5
- Molecular Weight:907.80
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Storage:
-20°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) INY-03-041 trihydrochloride
MoreAll PROTACs Isoforms
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Biological Activity
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Akt1 2.0 nM (IC50) |
Akt3 3.5 nM (IC50) |
Akt2 6.8 nM (IC50) |
Cereblon |
INY-03-041 (10-1000 nM; 0-24 hours) induces potent degradation of all three AKT isoforms in MDA-MB-468 cells[1].
INY-03-041 exhibits potent in vitro inhibition of S6K1 (IC50 =37.3 nM) and PKG1 (IC50 = 33.2 nM)[1].
INY-03-041 displays enhanced anti-proliferative effects compared with Ipatasertib (HY-15186) in MDA-MB-468 and HCC1937 cells[1].
INY-03-041 (250 nM, 12 h) promotes sustained AKT degradation and inhibition of downstream signaling effects for up to 96 h, even after compound washout[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-468 cells
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Concentration:0, 10, 50, 100, 250, 500, and 1000 nM
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Incubation Time:0, 2, 4, 6, 8. 10, 12, and 24 h
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Result:Induced potent degradation of all three AKT isoforms in a dose-dependent manner after a 12-h treatment, with maximal degradation observed between 100 and 250 nM. At concentrations of 500 nM and greater, AKT degradation is diminished. Treatment with 250 nM of INY-03-041 over time reveals partial degradation of all AKT isoforms within 4 h and progressive loss of AKT abundance out to 24 h.
Chemical Information
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Appearance Solid
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Molecular Weight 907.80
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Formula C44H59Cl4N7O5
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Color Off-white to light yellow
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SMILES
O=C(C(N(CC1=C2C=CC=C1CCCCCCCCCCNC[C@H](C3=CC=C(Cl)C=C3)C(N4CCN(C5=C([C@H](C)C[C@H]6O)C6=NC=N5)CC4)=O)C2=O)CC7)NC7=O.Cl.Cl.Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Publications (1)
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Journal Impact Factor
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Most Recent
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ACS Omega
Dynamic Detection of the E3-PROTAC-Target Protein Ternary Complex In Vitro and In Vivo via Bimolecular Fluorescence Complementation. [Abstract]2024 Dec 3;9(50):49739-49748. PMID: 39713624
Solvent & Solubility
DMSO : 100 mg/mL (110.16 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (272 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. You I, et al. Discovery of an AKT Degrader with Prolonged Inhibition of Downstream Signaling. Cell Chem Biol. 2020 Jan 16;27(1):66-73.e7. [Content Brief]
[2]. Maira SM, et al. Identification and characterization of NVP-BKM120, an orally available pan-class I PI3-kinase inhibitor. Mol Cancer Ther. 2012 Feb;11(2):317-28. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 1.1016 mL | 5.5078 mL | 11.0156 mL | 27.5391 mL |
| 5 mM | 0.2203 mL | 1.1016 mL | 2.2031 mL | 5.5078 mL | |
| 10 mM | 0.1102 mL | 0.5508 mL | 1.1016 mL | 2.7539 mL | |
| 15 mM | 0.0734 mL | 0.3672 mL | 0.7344 mL | 1.8359 mL | |
| 20 mM | 0.0551 mL | 0.2754 mL | 0.5508 mL | 1.3770 mL | |
| 25 mM | 0.0441 mL | 0.2203 mL | 0.4406 mL | 1.1016 mL | |
| 30 mM | 0.0367 mL | 0.1836 mL | 0.3672 mL | 0.9180 mL | |
| 40 mM | 0.0275 mL | 0.1377 mL | 0.2754 mL | 0.6885 mL | |
| 50 mM | 0.0220 mL | 0.1102 mL | 0.2203 mL | 0.5508 mL | |
| 60 mM | 0.0184 mL | 0.0918 mL | 0.1836 mL | 0.4590 mL | |
| 80 mM | 0.0138 mL | 0.0688 mL | 0.1377 mL | 0.3442 mL | |
| 100 mM | 0.0110 mL | 0.0551 mL | 0.1102 mL | 0.2754 mL |
INY-03-041 trihydrochloride Related Classifications
HY-133120A Related Classifications
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