AT7519 TFA
Based on 18 publication(s) in Google Scholar
AT7519 (AT7519M) TFA as 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.
For research use only. We do not sell to patients.
- Purity: 99.75%
- CAS No.: 1431697-85-6
- Formula: C18H18Cl2F3N5O4
- Molecular Weight:496.27
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Storage:
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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) AT7519 TFA
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
Biological Activity
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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) |
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Cell Line
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Type | Value | Description | References |
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| MV4-11 | EC50 |
1.1 μM
Compound: 11; AT7519
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Anticancer activity against human MV4-11 cells assessed as cell growth inhibition for 6 hrs followed by compound washout measured after 24 hrs by Annexin V/Propidium iodide staining based flow cytometric analysis
Anticancer activity against human MV4-11 cells assessed as cell growth inhibition for 6 hrs followed by compound washout measured after 24 hrs by Annexin V/Propidium iodide staining based flow cytometric analysis
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[PMID: 37071962] |
AT7519 (0-4 μM) TFA 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 TFA overcomes proliferative advantage conferred by cytokines and the protective effect of BMSC. AT7519 (0.5 μM) TFA induces apoptosis of MM cells in a time-dependent manner. Moreover, AT7519 (0.5 μM) TFA inhibits phosphorylation of RNA polymerase II CTD and partially inhibits RNA synthesis in MM.1S cells[1]. AT7519 (250 nM) TFA inhibits cell cycle progression in human tumor cell lines. AT7519 TFA also induces apoptosis of human tumor cell lines[2]. AT7519 (100-700 nM) TFA induces apoptosis in leukemia cell lines. AT7519TFA also inhibits transcription in human tumor cell lines. Furthermore, AT7519 TFA 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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1431697-85-6
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Appearance Solid
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Molecular Weight 496.27
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Formula C18H18Cl2F3N5O4
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Color White to gray
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SMILES
O=C(NC1=CNN=C1C(NC2CCNCC2)=O)C3=C(Cl)C=CC=C3Cl.O=C(O)C(F)(F)F
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Synonyms
AT7519M TFA
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
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 TFA 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 TFA 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 TFA 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 TFA 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 TFA 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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Solvent & Solubility
DMSO : 100 mg/mL (201.50 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). 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). 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)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.04 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.04 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
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.
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.
Purity & Documentation
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Data Sheet (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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Handling Instructions (2659 KB)
References
[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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0150 mL | 10.0752 mL | 20.1503 mL | 50.3758 mL |
| 5 mM | 0.4030 mL | 2.0150 mL | 4.0301 mL | 10.0752 mL | |
| 10 mM | 0.2015 mL | 1.0075 mL | 2.0150 mL | 5.0376 mL | |
| 15 mM | 0.1343 mL | 0.6717 mL | 1.3434 mL | 3.3584 mL | |
| 20 mM | 0.1008 mL | 0.5038 mL | 1.0075 mL | 2.5188 mL | |
| 25 mM | 0.0806 mL | 0.4030 mL | 0.8060 mL | 2.0150 mL | |
| 30 mM | 0.0672 mL | 0.3358 mL | 0.6717 mL | 1.6792 mL | |
| 40 mM | 0.0504 mL | 0.2519 mL | 0.5038 mL | 1.2594 mL | |
| 50 mM | 0.0403 mL | 0.2015 mL | 0.4030 mL | 1.0075 mL | |
| 60 mM | 0.0336 mL | 0.1679 mL | 0.3358 mL | 0.8396 mL | |
| 80 mM | 0.0252 mL | 0.1259 mL | 0.2519 mL | 0.6297 mL | |
| 100 mM | 0.0202 mL | 0.1008 mL | 0.2015 mL | 0.5038 mL |
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