Cat. No.: HY-130247

Flonoltinib

(Synonyms: JAK2/FLT3-IN-1)

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Flonoltinib is a potent and orally active dual JAK2/FLT3 inhibitor with IC₅₀ values of 0.7 nM, 4 nM, 26 nM and 39 nM for JAK2, FLT3, JAK1 and JAK3, respectively. Flonoltinib has anti-cancer activity.

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Pureté: 99.48%
CAS No.: 2387765-27-5
Formule: C₂₅H₃₄FN₇O
Masse moléculaire:467.58

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Flonoltinib Chemical Structure

CAS No.: 2387765-27-5

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Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target^[1]

JAK2

0.7 nM (IC₅₀)

FLT3

4 nM (IC₅₀)

JAK1

26 nM (IC₅₀)

JAK3

39 nM (IC₅₀)

Voir tous les produits spécifiques à Isoform JAK :

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	IC₅₀	145 nM Compound: 18e	Inhibition of JAK2 V617F mutant in BAF3 cells assessed as reduction in cell growth measured after 72 hrs by MTT assay Inhibition of JAK2 V617F mutant in BAF3 cells assessed as reduction in cell growth measured after 72 hrs by MTT assay	[PMID: 31670517]
MOLM-13	IC₅₀	72 nM Compound: 18e	Antiproliferative activity against FLT3-ITD-positive human MOLM13 cells assessed as reduction in cell growth after 72 hrs by MTT assay Antiproliferative activity against FLT3-ITD-positive human MOLM13 cells assessed as reduction in cell growth after 72 hrs by MTT assay	[PMID: 31670517]
MV4-11	IC₅₀	5.3 nM Compound: 18e	Antiproliferative activity against FLT3-ITD-positive human MV4-11 cells assessed as reduction in cell growth after 72 hrs by MTT assay Antiproliferative activity against FLT3-ITD-positive human MV4-11 cells assessed as reduction in cell growth after 72 hrs by MTT assay	[PMID: 31670517]
SET-2	IC₅₀	270 nM Compound: 18e	Antiproliferative activity against human SET2 cells overexpressing JAK2 V716F mutant assessed as reduction in cell growth after 72 hrs by MTT assay Antiproliferative activity against human SET2 cells overexpressing JAK2 V716F mutant assessed as reduction in cell growth after 72 hrs by MTT assay	[PMID: 31670517]
TF-1	IC₅₀	269.9 nM Compound: 18e	Inhibition of JAK2 in human TF-1 cells assessed as reduction in IL-3-induced STAT5 phosphorylation by flow cytometry Inhibition of JAK2 in human TF-1 cells assessed as reduction in IL-3-induced STAT5 phosphorylation by flow cytometry	[PMID: 31670517]
TF-1	IC₅₀	692.1 nM Compound: 18e	Inhibition of JAK1 in human TF-1 cells assessed as reduction in IL-6-induced STAT3 phosphorylation by flow cytometry Inhibition of JAK1 in human TF-1 cells assessed as reduction in IL-6-induced STAT3 phosphorylation by flow cytometry	[PMID: 31670517]
THP-1	IC₅₀	578.4 nM Compound: 18e	Inhibition of JAK1/JAK3 in human THP-1 cells assessed as reduction in IL-4-induced STAT6 phosphorylation by flow cytometry Inhibition of JAK1/JAK3 in human THP-1 cells assessed as reduction in IL-4-induced STAT6 phosphorylation by flow cytometry	[PMID: 31670517]

In Vitro

Flonoltinib (0.008-1 μM; for 2 hours) down-regulates p-FLT3 in a dose-dependent manner^[1].
Flonoltinib (5-100 nM; for 2 hours) has a dose-dependent effect on the induction of apoptosis in the MV4-11 cells^[1].
Flonoltinib (5-100 nM; for 2 hours) strongly induces cell cycle arrest with a G1/G0 percentage of 85% at 100 nM in the MV4-11 cells^[1].

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

Western Blot Analysis^[1]

Cell Line:

MV4-11 and SET-2 cells
Concentration:

0.008, 0.04, 0.2, 1 μM
Incubation Time:

For 2 hours
Result:

Down-regulated p-FLT3 in a dose-dependent manner from 0.008 to 1 μM.

Apoptosis Analysis^[1]

Cell Line:

MV4-11 cells
Concentration:

5, 10, 50, 100 nM
Incubation Time:

For 2 hours
Result:

Had a dose-dependent effect on the induction of apoptosis in the MV4-11 cells.

Cell Cycle Analysis^[1]

Cell Line:

MV4-11 cells
Concentration:

5, 10, 50, 100 nM
Incubation Time:

For 2 hours
Result:

Induced cell cycle arrest with a G1/G0 percentage of 85% at 100 nM.

In Vivo

Flonoltinib (30 and 60 mg/kg/day; p.o.; for 14 days) exhibits significant antitumor effects^[1].

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

Animal Model:

NOD/SCID mouse models^[1]
Dosage:

30 and 60 mg/kg
Administration:

Oral administration; daily; for 14 days
Result:

Exhibited significant antitumor effects.
The tumor growth inhibitory rates (TGI) were respective 58% and 93% in the MV4-11-bearing mice model.

Chemical Information

CAS No. 2387765-27-5
Appearance Solid
Masse moléculaire 467.58
Formule C₂₅H₃₄FN₇O
Color White to off-white
SMILES

OCCN(C1CCN(C2=CC=C(NC3=NC=C(C)C(C4=CN(C(C)C)N=C4)=N3)C=C2F)CC1)C
Synonyms

JAK2/FLT3-IN-1
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (1)

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Journal Impact Factor

J Immunol

Tumor Environment Promotes Lnc57Rik-Mediated Suppressive Function of Myeloid-Derived Suppressor Cells. [Abstract]

2022 Oct 1;209(7):1401-1413. PMID: 36038289

Solvant et solubilité

In Vitro:

DMSO : 35 mg/mL (74.85 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

2.1387 mL

10.6934 mL

21.3867 mL

5 mM

0.4277 mL

2.1387 mL

4.2773 mL

10 mM

0.2139 mL

1.0693 mL

2.1387 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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: 2.08 mg/mL (4.45 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.08 mg/mL (4.45 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (274 KB)
SDS (251 KB)
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- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
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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)
Instruction de manipulation (2659 KB)

Références

[1]. Yang T, et al. Discovery of Potent and Orally Effective Dual JAK2/FLT3 Inhibitors for the Treatment of AcuteMyelogenous Leukemia and Myeloproliferative Neoplasms. J Med Chem. 2019 Oct 31. [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, 6 months; -20°C, 1 month. 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	2.1387 mL	10.6934 mL	21.3867 mL	53.4668 mL
	5 mM	0.4277 mL	2.1387 mL	4.2773 mL	10.6934 mL
	10 mM	0.2139 mL	1.0693 mL	2.1387 mL	5.3467 mL
	15 mM	0.1426 mL	0.7129 mL	1.4258 mL	3.5645 mL
	20 mM	0.1069 mL	0.5347 mL	1.0693 mL	2.6733 mL
	25 mM	0.0855 mL	0.4277 mL	0.8555 mL	2.1387 mL
	30 mM	0.0713 mL	0.3564 mL	0.7129 mL	1.7822 mL
	40 mM	0.0535 mL	0.2673 mL	0.5347 mL	1.3367 mL
	50 mM	0.0428 mL	0.2139 mL	0.4277 mL	1.0693 mL
	60 mM	0.0356 mL	0.1782 mL	0.3564 mL	0.8911 mL

Keywords

Flonoltinib

1 Cited Publications

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Flonoltinib

Apoptosis Compound Library

Epigenetics Compound Library

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Stem Cell Signaling Compound Library

Anti-Cancer Compound Library

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Differentiation Inducing Compound Library

Reprogramming Compound Library

Orally Active Compound Library

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Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

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Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Pain-Related Compound Library

Membrane Protein-targeted Compound Library

Autoimmune Disease Compound Library

Cytokine Inhibitors Library

Cell Death Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Brain Cancer Compound Library

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Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) Flonoltinib

Voir tous les produits spécifiques à Isoform JAK

Activité biologique

Chemical Information

Publications (1)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Flonoltinib Related Classifications

HY-130247 Related Classifications