Gandotinib
Based on 4 publication(s) in Google Scholar
Gandotinib (LY2784544) is a potent JAK2 inhibitor with IC50 of 3 nM. Gandotinib (LY2784544) also inhibits FLT3, FLT4, FGFR2, TYK2, and TRKB with IC50 of 4, 25, 32, 44, and 95 nM.
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- Pureté: 99.86%
- CAS No.: 1229236-86-5
- Formule: C23H25ClFN7O
- Masse moléculaire:469.94
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Activité biologique
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) Gandotinib
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Activité biologique
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JAK2 3 nM (IC50) |
Tyk2 44 nM (IC50) |
JAK3 48 nM (IC50) |
FGFR2 32 nM (IC50) |
FGFR3 106 nM (IC50) |
Flt-4 25 nM (IC50) |
KDR 109 nM (IC50) |
FLT3 4 nM (IC50) |
TRKB 95 nM (IC50) |
ALK 138 nM (IC50) |
MUSK 147 nM (IC50) |
AURKA 168 nM (IC50) |
MAP3K9 299 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BaF3 | IC50 |
1309 nM
Compound: 34
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Inhibition of cell proliferation in IL-3 stimulated mouse BaF3 cells expressing wild-type JAK2
Inhibition of cell proliferation in IL-3 stimulated mouse BaF3 cells expressing wild-type JAK2
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[PMID: 32120325] |
| BaF3 | IC50 |
55 nM
Compound: 34
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Inhibition of cell proliferation in mouse BaF3 cells expressing JAK2 V617F mutant
Inhibition of cell proliferation in mouse BaF3 cells expressing JAK2 V617F mutant
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[PMID: 32120325] |
Gandotinib (LY2784544), a potent, selective and ATP-competitive inhibitor of janus kinase 2 (JAK2) tyrosine kinase. LY2784544 effectively inhibits JAK2V617F-driven signaling and cell proliferation in Ba/F3 cells (IC50=20 and 55 nM, respectively). In comparison, Gandotinib (LY2784544) is much less potent at inhibiting interleukin-3-stimulated wild-type JAK2-mediated signaling and cell proliferation (IC50=1183 and 1309 nM, respectively). Gandotinib (LY2784544) potently inhibits the JAK2V617F signaling (IC50=20 nM) but, remarkably, shows very minimal activity against the IL-3-activated wild-type JAK2 signaling with an IC50 of 1183 nM. LY2784544 inhibits the proliferation of JAK2V617F-expressing cells (IC50=55 nM) and is markedly less potent as an inhibitor of the proliferation of IL-3-stimulated wild-type JAK2 expressing Ba/F3 cells (IC50=1309 nM). Gandotinib (LY2784544) is potent in the cell-based TF-1 JAK2 assay (IC50=45 nM) and had the desired threshold selectivity in the NK-92 JAK3/JAK1 heterodimer assay (942 nM)[1].
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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1229236-86-5
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Appearance Solid
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Masse moléculaire 469.94
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Formule C23H25ClFN7O
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Color Light yellow to yellow
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SMILES
CC1=NNC(NC2=NN3C(C(CN4CCOCC4)=C2)=NC(C)=C3CC5=CC=C(C=C5F)Cl)=C1
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Synonyms
LY2784544
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (4)
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Journal Impact Factor
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Most Recent
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Nat Commun
Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]2026 Feb 12;17(1):1214. PMID: 41680175 -
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 -
Biol Pharm Bull
2019 Aug 1;42(8):1415-1418. PMID: 31167986
Gandotinib purchased from MedChemExpress. Usage Cited in: Biol Pharm Bull. 2019 Aug 1;42(8):1415-1418. [Abstract]
TC-G 1008 (10 μM) and LY2784544 (1 μM) suppress IL-6 production in U937 macrophage cells; culture supernatants were collected 6 h after LPS stimulation.
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Solvant et solubilité
DMSO : 33.33 mg/mL (70.92 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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 (5.32 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.
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.
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.
Protocole
Ba/F3 cells expressing JAK2V617F are placed in RPMI-1640-containing vehicle (DMSO) or Gandotinib (LY2784544) (concentration range, 0.001-20 μM) (1×104 cells/96-well). Ba/F3 cells expressing wild-type JAK2 are treated similarly except IL-3 (2 ng/mL) is added. After a 72-hour incubation, cell proliferation is assessed by adding Cell Titer 96 Aqueous One Solution Reagent (20 μL/well). The IC50 for inhibition of cell proliferation is calculated using the GraphPad Prism 4 software[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[1]
Dose- and time-dependent in vivo inhibition of JAK2V617F signaling is assessed by measuring inhibition of STAT5 phosphorylation in a mouse ascitic tumor model. Ba/F3-JAK2V617F-GFP cells (1×107) are implanted in the intraperitoneal cavity of severe combined immunodeficiency mice (SCID mice) and allowed to develop into ascitic tumors for 7 days. For dose-response studies (six animals/group), Gandotinib (LY2784544) is administered once by oral gavage (2.5, 5, 10, 20, 40, or 80 mg/kg), then 30 min later, ascitic tumor cells are collected, fixed, incubated for 2 h with Mouse-anti-pSTAT5 (pY694) Alexa Fluor 647 (1:10 dilution), and analyzed by flow cytometry. Time course studies are performed similarly, except the animals are treated with Gandotinib (LY2784544) at 20, 40 or 80 mg/kg and ascitic tumor cells collected at prespecified intervals of 0.25-6 h after dosing. Data are analyzed by the one-way analysis of variance, and Dunnett's test (α=0.05). Dose response data are analyzed with a four-parameter logistic curve-fitting program.
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)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1279 mL | 10.6397 mL | 21.2793 mL | 53.1983 mL |
| 5 mM | 0.4256 mL | 2.1279 mL | 4.2559 mL | 10.6397 mL | |
| 10 mM | 0.2128 mL | 1.0640 mL | 2.1279 mL | 5.3198 mL | |
| 15 mM | 0.1419 mL | 0.7093 mL | 1.4186 mL | 3.5466 mL | |
| 20 mM | 0.1064 mL | 0.5320 mL | 1.0640 mL | 2.6599 mL | |
| 25 mM | 0.0851 mL | 0.4256 mL | 0.8512 mL | 2.1279 mL | |
| 30 mM | 0.0709 mL | 0.3547 mL | 0.7093 mL | 1.7733 mL | |
| 40 mM | 0.0532 mL | 0.2660 mL | 0.5320 mL | 1.3300 mL | |
| 50 mM | 0.0426 mL | 0.2128 mL | 0.4256 mL | 1.0640 mL | |
| 60 mM | 0.0355 mL | 0.1773 mL | 0.3547 mL | 0.8866 mL |
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