Art. -Nr.: HY-13034

Gandotinib

(Synonyms: LY2784544)

4 Cited Publications

Kundenbewertung

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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Reinheit: 99.86%
CAS. Nr.: 1229236-86-5
Formel: C₂₃H₂₅ClFN₇O
Molecular Weight:469.94

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Gandotinib Chemical Structure

CAS. Nr.: 1229236-86-5

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (4)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Bioz

Biologische Aktivität

Beschreibung

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.

IC₅₀ & Target^[1]

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)

Alle JAK Isoform-spezifische Produkte anzeigen :

Alle VEGFR Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	IC₅₀	1309 nM Compound: 34	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	[PMID: 32120325]
BaF3	IC₅₀	55 nM Compound: 34	Inhibition of cell proliferation in mouse BaF3 cells expressing JAK2 V617F mutant Inhibition of cell proliferation in mouse BaF3 cells expressing JAK2 V617F mutant	[PMID: 32120325]

In Vitro

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.

In Vivo

Gandotinib (LY2784544) effectively inhibits STAT5 phosphorylation in Ba/F3-JAK2V617F-GFP (green fluorescent protein) ascitic tumor cells (TED₅₀=12.7 mg/kg) and significantly reduces (P<0.05) Ba/F3-JAK2V617F-GFP tumor burden in the JAK2V617F-induced MPN model (TED₅₀=13.7 mg/kg, twice daily)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 1229236-86-5
Appearance Solid
Molecular Weight 469.94
Formel C₂₃H₂₅ClFN₇O
Color Light yellow to yellow
SMILES

CC1=NNC(NC2=NN3C(C(CN4CCOCC4)=C2)=NC(C)=C3CC5=CC=C(C=C5F)Cl)=C1
Synonyms

LY2784544
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

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

G Protein-Coupled Receptor 39 Agonist Improves Concanavalin A-Induced Hepatitis in Mice. [Abstract]

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.
Patent

US20180263995A1.

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.1279 mL

10.6397 mL

21.2793 mL

5 mM

0.4256 mL

2.1279 mL

4.2559 mL

10 mM

0.2128 mL

1.0640 mL

2.1279 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass

Konzentration

Volumen

Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.32 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage
mg/kg
Animal Weight (Per Animal)
g
Dosing Volume (Per Animal)
μL
Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Protokoll

Cell Assay^[1]

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.

Animal Administration^[1]

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.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (285 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Ma L, et al. Discovery and characterization of LY2784544, a small-molecule tyrosine kinase inhibitor of JAK2V617F. Blood Cancer J. 2013, 3, e109. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

Gandotinib

4 Cited Publications

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Gandotinib

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Publications Citing Use of MedChemExpress (MCE) Gandotinib

Alle JAK Isoform-spezifische Produkte anzeigen

Alle VEGFR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (4)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Gandotinib Related Classifications

Art. -Nr.: HY-13034