AT7519 Hydrochloride
Based on 18 publication(s) in Google Scholar
AT7519 Hydrochloride is a potent inhibitor of CDKs, with IC50s of 210, 47, 100, 13, 170, and <10 nM for CDK1, CDK2, CDK4 to CDK6, and CDK9, respectively.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté : 99.16%
- CAS No.: 902135-91-5
- Formule: C16H18Cl3N5O2
- Masse moléculaire:418.71
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Stockage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) AT7519 Hydrochloride
More- Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. [Abstract]
- Adv Sci (Weinh). 2024 Mar;11(11):e2305260. [Abstract]
- Cell Rep Med. 2026 May 14:102819. [Abstract]
- Oncogene. 2023 Nov;42(47):3503-3513. [Abstract]
- Cell Chem Biol. 2018 Feb 15;25(2):135-142.e5. [Abstract]
- EMBO Mol Med. 2025 Nov 26. [Abstract]
- Sci Rep. 2021 Mar 8;11(1):5374. [Abstract]
- FASEB J. 2024 Apr 30;38(8):e23628. [Abstract]
- FEBS J. 2026 May 4. [Abstract]
- RNA Biol. 2021 Nov 12;18(sup2):722-729. [Abstract]
- Mol Carcinog. 2025 Dec 2. [Abstract]
- Glycobiology. 2022 Aug 18;32(9):751-759. [Abstract]
- Exp Eye Res. 2023 Feb:227:109391. [Abstract]
- PLoS One. 2025 Jun 17;20(6):e0324443. [Abstract]
- Dev Biol. 2024 Apr:508:93-106. [Abstract]
- SSRN. 2026 May 20.
- bioRxiv. 2025 Nov 17.
- bioRxiv. 2024 September 07.
Customer Validation & Images
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WB
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RT-PCR
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Cell Proliferation/Viability Assay
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IP
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WB
Activité biologique
Description
IC50 & Target
[2]|
CDK9/Cyclin T 10 nM (IC50) |
CDK5/p35 13 nM (IC50) |
cdk2/cyclin A 47 nM (IC50) |
Cdk4/cyclin D1 100 nM (IC50) |
cdk6/cyclin D3 170 nM (IC50) |
Cdk1/cyclin B 210 nM (IC50) |
CDK7/Cyclin H/MAT1 2400 nM (IC50) |
GSK3β 89 nM (IC50) |
In Vitro
AT7519 (0-4 μM) results in dose-dependent cytotoxicity with IC50s ranging from 0.5 to 2 μM in MM cells, and this induced cytotoxicity is associated with GSK-3β activation independent of transcriptional inhibition. AT7519 overcomes proliferative advantage conferred by cytokines and the protective effect of BMSC. AT7519 (0.5 μM) induces apoptosis of MM cells in a time-dependent manner. Moreover, AT7519 (0.5 μM) inhibits phosphorylation of RNA polymerase II CTD and partially inhibits RNA synthesis in MM.1S cells[1]. AT7519 (250 nM) inhibits cell cycle progression in human tumor cell lines. AT7519 also induces apoptosis of human tumor cell lines[2]. AT7519 (100-700 nM) induces apoptosis in leukemia cell lines. AT7519 also inhibits transcription in human tumor cell lines. Furthermore, AT7519 inhibits RNA polymerase II and reduces antiapoptotic protein levels[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 902135-91-5
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Appearance Solid
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Masse moléculaire 418.71
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Formule C16H18Cl3N5O2
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Color White to off-white
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SMILES
O=C(C(C(Cl)=CC=C1)=C1Cl)NC2=CNN=C2C(NC3CCNCC3)=O.[H]Cl
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (18)
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Journal Impact Factor
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Most Recent
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Sci Transl Med
PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]2018 Jul 18;10(450):eaaq1093. PMID: 30021885 -
Adv Sci (Weinh)
SHMT2 Mediates Small-Molecule-Induced Alleviation of Alzheimer Pathology Via the 5'UTR-dependent ADAM10 Translation Initiation. [Abstract]2024 Mar;11(11):e2305260. PMID: 38183387
AT7519 Hydrochloride purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2024 Mar;11(11):e2305260. [Abstract]
Chemical structure of another CDK/GSK inhibitor AT7519 (top), and immunoblots (middle) and quantification (bottom) of ADAM10 in SH‐SY5Y cells treated with AT7519 (1 to 20 µM for 36 h, n = 5)
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Cell Rep Med
Artificial exosomes synergistically reshape sepsis immune homeostasis by modulating neutrophil fate and blocking PD-1/PD-L1. [Abstract]2026 May 14:102819. PMID: 42140195 -
Oncogene
D-mannose induces TFE3-dependent lysosomal degradation of EGFR and inhibits the progression of NSCLC. [Abstract]2023 Nov;42(47):3503-3513. PMID: 37845392
AT7519 Hydrochloride purchased from MedChemExpress. Usage Cited in: Oncogene. 2023 Nov;42(47):3503-3513. [Abstract]
Western blot analysis of the levels of pGSK3β (S9), GSK3β and EGFR in A549 and PC9 cells treated with AT7519 (0.5 μM, 30 h), DIF-3 (30 μM, 30 h) and D-mannose (25 mM, 24 h) as indicated.
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Cell Chem Biol
2018 Feb 15;25(2):135-142.e5. PMID: 29276047 -
EMBO Mol Med
Isomeranzin activates Gnas-AMPK signaling to drive white adipose browning and curb obesity in mice. [Abstract]2025 Nov 26. PMID: 41299101 -
Sci Rep
2021 Mar 8;11(1):5374. PMID: 33686114 -
FASEB J
2024 Apr 30;38(8):e23628. PMID: 38661032
AT7519 Hydrochloride purchased from MedChemExpress. Usage Cited in: FASEB J. 2024 Apr 30;38(8):e23628. [Abstract]
RT-qPCR data analysis showing the on-target effect of CDK9 inhibition (500 nM AT7519 for 4 h) on MYC mRNA.
AT7519 Hydrochloride purchased from MedChemExpress. Usage Cited in: FASEB J. 2024 Apr 30;38(8):e23628. [Abstract]
Cell viability was measured using CellTiter-Glo after 4 days of treatment with mTOR inhibitor (everolimus) in the presence or absence of AT7519 (LNCaP and C4-2: 0.5 μM; 22RV1: 2 μM).
AT7519 Hydrochloride purchased from MedChemExpress. Usage Cited in: FASEB J. 2024 Apr 30;38(8):e23628. [Abstract]
LNCaP cells were treated with a CDK9 inhibitor (500 nM AT7519) for 4 h, and wheat germ agglutinin (WGA)-lectin pulldown was used to enrich for proteins O-GlcNAcylated in the given conditions. The data are representative of two biological replicates; OGT is used as a positive control andactin as a negative control in the pulldown samples. For clarity, both long- and short- exposure Western blots of MAVS antibody are shown. Densitometry was used to determine the signal intensities.
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FEBS J
CDK14 is a critical regulator of haematopoietic stem and progenitor cell maintenance and post-transplantation proliferation. [Abstract]2026 May 4. PMID: 42080702 -
RNA Biol
2021 Nov 12;18(sup2):722-729. PMID: 34592899 -
Mol Carcinog
Purvalanol A Exerts Anti-Hepatocellular Carcinoma Activity by Activating the p53 Pathway. [Abstract]2025 Dec 2. PMID: 41328606 -
Glycobiology
2022 Aug 18;32(9):751-759. PMID: 35708495 -
Exp Eye Res
2023 Feb:227:109391. PMID: 36696946 -
PLoS One
2025 Jun 17;20(6):e0324443. PMID: 40526635 -
Dev Biol
Neutrophils facilitate the epicardial regenerative response after zebrafish heart injury. [Abstract]2024 Apr:508:93-106. PMID: 38286185 -
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Solvant et solubilité
In Vitro:
DMSO : ≥ 300 mg/mL (716.49 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 8.33 mg/mL (19.89 mM; Need ultrasonic)
* "≥" means soluble, but saturation unknown.
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). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocole
Cell Assay[1]
AT7519's effects on viability of MM cell lines, primary MM cells, and PBMNCs is assessed by measuring 3-(4,5-dimethylthiazol-2-yl)-2,5 diphenyl tetrasodium bromide (MTT) dye absorbance. DNA synthesis is measured by tritiated thymidine uptake (3H-TdR). MM cells (2-3 × 104 cells/well) are incubated in 96-well culture plates with media and different concentrations of AT7519 and/or recombinant IL-6 (10 ng/mL) or IGF-1 (50 ng/mL) for 24 or 48 h at 37°C and 3H-TdR incorporation is measured.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration[1]
To evaluate the in vivo anti-MM activity of AT7519, male SCID mice are inoculated subcutaneously with 5×106 MM.1S cells in 100 μL serum-free RPMI 1640 medium. When tumors are measurable, mice are treated intraperitoneally (IP) with vehicle or AT7519 dissolved in saline 0.9%. The first group of 10 mice is treated with 15 mg/kg once a day for five days for 2 weeks, and the second group is treated with 15 mg/kg once a day three times a week for four consecutive weeks. The control group receives the carrier alone at the same schedule. Tumor size is measured every alternate day in 2 dimensions using calipers, and tumor volume is calculated with the formula: V= 0.5 a × b2 (a= long diameter of the tumor, b= short diameter of the tumor). Animals are sacrificed when the tumor reaches 2 cm3 or when the tumor is ulcerated. Survival and tumor growth are evaluated from the first day of treatment until death.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (285 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Santo L, et al. AT7519, A novel small molecule multi-cyclin-dependent kinase inhibitor, induces apoptosis in multiple myeloma via GSK-3beta activation and RNA polymerase II inhibition. Oncogene. 2010 Apr 22;29(16):2325-36. [Content Brief]
[2]. Squires MS, et al. Biological characterization of AT7519, a small-molecule inhibitor of cyclin-dependent kinases, in human tumor cell lines. Biological characterization of AT7519, a small-molecule inhibitor of cyclin-dependent kinases, in human tumor cell lines. [Content Brief]
[3]. Squires MS, et al. AT7519, a cyclin-dependent kinase inhibitor, exerts its effects by transcriptional inhibition in leukemia cell lines and patient samples. Mol Cancer Ther. 2010 Apr;9(4):920-8. [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). 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 |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 2.3883 mL | 11.9414 mL | 23.8829 mL | 59.7072 mL |
| 5 mM | 0.4777 mL | 2.3883 mL | 4.7766 mL | 11.9414 mL | |
| 10 mM | 0.2388 mL | 1.1941 mL | 2.3883 mL | 5.9707 mL | |
| 15 mM | 0.1592 mL | 0.7961 mL | 1.5922 mL | 3.9805 mL | |
| DMSO | 20 mM | 0.1194 mL | 0.5971 mL | 1.1941 mL | 2.9854 mL |
| 25 mM | 0.0955 mL | 0.4777 mL | 0.9553 mL | 2.3883 mL | |
| 30 mM | 0.0796 mL | 0.3980 mL | 0.7961 mL | 1.9902 mL | |
| 40 mM | 0.0597 mL | 0.2985 mL | 0.5971 mL | 1.4927 mL | |
| 50 mM | 0.0478 mL | 0.2388 mL | 0.4777 mL | 1.1941 mL | |
| 60 mM | 0.0398 mL | 0.1990 mL | 0.3980 mL | 0.9951 mL | |
| 80 mM | 0.0299 mL | 0.1493 mL | 0.2985 mL | 0.7463 mL | |
| 100 mM | 0.0239 mL | 0.1194 mL | 0.2388 mL | 0.5971 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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