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

Name: Flonoltinib
Brand: MedChemExpress
SKU: HY-130247
Rating: 4.5 (1 reviews)

Cat. No.: HY-130247 Purity: 99.79%: FAQs
Data Sheet SDS COA Handling Instructions

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JAK2/FLT3-IN-1 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. JAK2/FLT3-IN-1 has anti-cancer activity.

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

Flonoltinib Chemical Structure

CAS No. : 2387765-27-5

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 772	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 772	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 750	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 1250	In-stock	Estimated Time of Arrival: December 31
50 mg		Get quote
100 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Flonoltinib:

Flonoltinib TFA Get quote
Flonoltinib monomaleate Get quote

1 Publications Citing Use of MCE Flonoltinib

•J Immunol. 2022 Aug 29;ji2200195. [Abstract]

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JAK1 JAK2 JAK3 Tyk2 JAK

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

JAK2

0.7 nM (IC₅₀)

FLT3

4 nM (IC₅₀)

JAK1

26 nM (IC₅₀)

JAK3

39 nM (IC₅₀)

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

JAK2/FLT3-IN-1 (0.008-1 μM; for 2 hours) down-regulates p-FLT3 in a dose-dependent manner^[1].
JAK2/FLT3-IN-1 (5-100 nM; for 2 hours) has a dose-dependent effect on the induction of apoptosis in the MV4-11 cells^[1].
JAK2/FLT3-IN-1 (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

JAK2/FLT3-IN-1 (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.

Molecular Weight

467.58

Formula

C₂₅H₃₄FN₇O

CAS No.

2387765-27-5

Appearance

Solid

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

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

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

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

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

Purity & Documentation

Purity: 99.79%

Select Batch:

Data Sheet (274 KB) SDS (251 KB)

COA (244 KB) HNMR (147 KB) RP-HPLC (244 KB) LCMS (105 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]

Complete Stock Solution Preparation Table

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

Flonoltinib Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Flonoltinib2387765-27-5JAK2/FLT3-IN-1JAKFLT3ApoptosisJanus kinaseCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3orallyanti-cancercyclearrestG1/G0MV4-11Inhibitorinhibitorinhibit

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

Customer Review

Other Forms of Flonoltinib:

Flonoltinib Related Antibodies

1 Publications Citing Use of MCE Flonoltinib

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•Related Screening Libraries:

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View All JAK Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Flonoltinib Related Antibodies

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Dilution Calculator

Complete Stock Solution Preparation Table

Flonoltinib Related Classifications

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