Cat. No.: HY-130247A

Flonoltinib TFA

(Synonyms: JAK2/FLT3-IN-1 TFA)

1 Cited Publications

Customer Review

Based on 1 publication(s) in Google Scholar

Flonoltinib TFA 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 TFA has anti-cancer activity.

For research use only. We do not sell to patients.

Purity: 98.04%
CAS No.: 2928093-29-0
Formula: C₂₇H₃₅F₄N₇O₃
Molecular Weight:581.61

Storage:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Flonoltinib TFA Chemical Structure

CAS No.: 2928093-29-0

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Fluorescent Dye

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

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (1)
Solvent & Solubility
- In Vitro
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

JAK1

26 nM (IC₅₀)

JAK2

0.7 nM (IC₅₀)

JAK3

39 nM (IC₅₀)

FLT3

4 nM (IC₅₀)

All JAK Isoforms :

In Vitro

Flonoltinib (0.008-1 μM; for 2 hours) TFA down-regulates p-FLT3 in a dose-dependent manner^[1].
Flonoltinib (5-100 nM; for 2 hours) TFA has a dose-dependent effect on the induction of apoptosis in the MV4-11 cells^[1].
Flonoltinib (5-100 nM; for 2 hours) TFA 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) TFA 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.

Clinical Trial

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

Chemical Information

CAS No. 2928093-29-0
Appearance Solid
Molecular Weight 581.61
Formula C₂₇H₃₅F₄N₇O₃
Color Yellow to orange
SMILES

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

JAK2/FLT3-IN-1 TFA
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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

Solvent & Solubility

In Vitro:

H₂O : 33.33 mg/mL (57.31 mM; Need ultrasonic)

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

1.7194 mL

8.5968 mL

17.1937 mL

5 mM

0.3439 mL

1.7194 mL

3.4387 mL

10 mM

0.1719 mL

0.8597 mL

1.7194 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 (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.

Molarity Calculator

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

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Dilution Calculator

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Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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)

References

[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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
H₂O	1 mM	1.7194 mL	8.5968 mL	17.1937 mL	42.9841 mL
	5 mM	0.3439 mL	1.7194 mL	3.4387 mL	8.5968 mL
	10 mM	0.1719 mL	0.8597 mL	1.7194 mL	4.2984 mL
	15 mM	0.1146 mL	0.5731 mL	1.1462 mL	2.8656 mL
	20 mM	0.0860 mL	0.4298 mL	0.8597 mL	2.1492 mL
	25 mM	0.0688 mL	0.3439 mL	0.6877 mL	1.7194 mL
	30 mM	0.0573 mL	0.2866 mL	0.5731 mL	1.4328 mL
	40 mM	0.0430 mL	0.2149 mL	0.4298 mL	1.0746 mL
	50 mM	0.0344 mL	0.1719 mL	0.3439 mL	0.8597 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.

Keywords

Flonoltinib TFA

1 Cited Publications

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Flonoltinib TFA

Apoptosis Compound Library

Epigenetics Compound Library

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

Kinase Inhibitor Library

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Publications Citing Use of MedChemExpress (MCE) Flonoltinib TFA

All JAK Isoforms

Biological Activity

Chemical Information

Publications (1)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Flonoltinib TFA Related Classifications

HY-130247A Related Classifications