2. Protein Tyrosine Kinase/RTK Apoptosis MAPK/ERK Pathway GPCR/G Protein PI3K/Akt/mTOR JAK/STAT Signaling Epigenetics Stem Cell/Wnt
  3. FLT3 Apoptosis Ras p38 MAPK PI3K Akt JAK STAT
  4. Clifutinib

Clifutinib is an orally active and selective internal tandem duplication mutation of FMS-like tyrosine kinase 3 (FLT3-ITD) inhibitor with an IC50 value of 15.1 nM. Clifutinib exerts strong antiproliferative effects on FLT3-ITD acute myeloid leukemia (AML) cell lines (MV-4-11: IC50 = 1.5 nM; MOLM-13: IC50 = 1.4 nM). Clifutinib inhibits the activity of FLT3-ITD kinase and blocks the downstream RAS/MAPK, PI3K/AKT, and JAK/STAT5 signaling pathways of FLT3. Clifutinib induces apoptosis of acute myeloid leukemia (AML) cells with FLT3-ITD mutations. Clifutinib demonstrates significant antitumor efficacy in mice bearing MV-4-11 or MOLM-13 xenografts. Clifutinib is promising for research of relapsed/refractory FLT3-ITD-positive acute myeloid leukemia.

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

Clifutinib

Clifutinib Chemical Structure

CAS No. : 1862226-99-0

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
5 mg In-stock
10 mg In-stock
25 mg In-stock
50 mg In-stock
100 mg In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Clifutinib Related Antibodies

Top Publications Citing Use of Products

View All Ras Isoform Specific Products:

View All Isoforms
K-Ras H-Ras N-Ras Ras

View All p38 MAPK Isoform Specific Products:

View All Isoforms
p38 MAPK p38α p38β MAPK13 p38δ p38γ

View All PI3K Isoform Specific Products:

View All Isoforms
PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

View All Akt Isoform Specific Products:

View All Isoforms
Akt Akt1 Akt2 Akt3

View All JAK Isoform Specific Products:

View All Isoforms
JAK1 JAK2 JAK3 Tyk2 JAK

View All STAT Isoform Specific Products:

View All Isoforms
STAT3 STAT5 STAT6 STAT1

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Clifutinib is an orally active and selective internal tandem duplication mutation of FMS-like tyrosine kinase 3 (FLT3-ITD) inhibitor with an IC50 value of 15.1 nM. Clifutinib exerts strong antiproliferative effects on FLT3-ITD acute myeloid leukemia (AML) cell lines (MV-4-11: IC50 = 1.5 nM; MOLM-13: IC50 = 1.4 nM). Clifutinib inhibits the activity of FLT3-ITD kinase and blocks the downstream RAS/MAPK, PI3K/AKT, and JAK/STAT5 signaling pathways of FLT3. Clifutinib induces apoptosis of acute myeloid leukemia (AML) cells with FLT3-ITD mutations. Clifutinib demonstrates significant antitumor efficacy in mice bearing MV-4-11 or MOLM-13 xenografts. Clifutinib is promising for research of relapsed/refractory FLT3-ITD-positive acute myeloid leukemia[1].

In Vitro

Clifutinib (72 h) shows anti-proliferative activities against MV-4-11 AML cells and MOLM-13 cells, with IC50s of 1.5 nM and 1.4 nM, respectively[1].
Clifutinib (9e, 0.1-1000 nM, 72 h) exhibits potent antiproliferative activity against Ba/F3 cells expressing FLT3 mutant isoforms, with IC50 values of 0.9 nM (Ba/F3-FLT3-ITD), 4.1 nM (Ba/F3-FLT3-ITD-D835A), 5.8 nM (Ba/F3-FLT3-ITD-D835G), 47.6 nM (Ba/F3-FLT3-ITD-D835Y), 74.7 nM (Ba/F3-FLT3-ITD-D835 Del), 130.0 nM (Ba/F3-FLT3-ITD-D835V), 2.9 nM (Ba/F3-FLT3-ITD-D835N), 301.9 nM (Ba/F3-FLT3-ITD-D835I), 6.9 nM (Ba/F3-FLT3-ITD-N676D), 25.0 nM (Ba/F3-FLT3-ITD-G697R), 38.0 nM (Ba/F3-FLT3-ITD-Y842H), 21.8 nM (Ba/F3-FLT3-ITD-Y842R), 154.0 nM (Ba/F3-FLT3-ITD-F691L), 154.4 nM (Ba/F3-FLT3-ITD-F691I), 5.4 nM (Ba/F3-FLT3-D835Y), 10.9 nM (Ba/F3-FLT3-D835H), 37.4 nM (Ba/F3-FLT3-D835V), while showing no antiproliferative effect on parental Ba/F3 cells with IC50 > 1000 nM[1].
Clifutinib (1-10 μM, 72 h) exhibits significant antiproliferative activity only against FLT3-ITD+ leukemia cell lines MV-4-11 and MOLM-13 with IC50 values of 0.0015 μM and 0.0014 μM, respectively, while showing minimal or no antiproliferative effects on FLT3-ITD-negative cell lines (RS4;11, HL-60, MOLT-4, RPMI8226, K562, NCI-H226, PC-3, DU 145, SK-OV-3, OVCAR-3, MCF-7, SW-620, COLO205, Caki-1, U87MG, U251) with IC50 > 10 μM, and weak activity against NCI-H460, A2780, HCT116, 786-O cells with IC50 values of 7.8 μM, 7.2 μM, 8.5 μM, 3.4 μM, respectively[1].
Clifutinib (1-100 nM, 48-72 h) induces apoptosis in MV-4-11 cells in a dose-dependent manner[1].
Clifutinib (1-1000 nM, 2 h) inhibits the phosphorylation of FLT3, ERK, AKT, and STAT5 in MV-4-11 cells in a dose-dependent manner without affecting total protein levels[1].

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

Clifutinib Related Antibodies

Apoptosis Analysis[1]

Cell Line: MV-4-11 cells
Concentration: 1, 3, 10, 30, 100 nM
Incubation Time: 48, 72 h
Result: Induced apoptosis in MV-4-11 cells in a dose-dependent manner.

Western Blot Analysis[1]

Cell Line: MV-4-11 cells
Concentration: 1, 3, 10, 30, 300, 1000 nM
Incubation Time: 2 h
Result: Inhibited the phosphorylation of FLT3, ERK, AKT, and STAT5 in MV-4-11 cells in a dose-dependent manner without affecting total protein levels.
In Vivo

Clifutinib (0.5-20 mg/kg, p.o., once daily, 8,10 or 21 days) demonstrates significant antitumor efficacy in NOD/SCID mice bearing MV-4-11 or MOLM-13 xenografts[1].

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

Animal Model: Human tumor xenografts were established by subcutaneous inoculation of mice (Female NOD/SCID or Balb/c nudemice (5-6 weeks old)) with MV-4-11 or MOLM-13 cells[1]
Dosage: 0.5, 1.5, 4.5, 20 mg/kg
Administration: p.o., once daily, 8, 10 or 21 days
Result: Achieved tumor growth inhibition.
Showed no significant changes in body weight.
Achieved complete inhibition of FLT3 and STAT5 phosphorylation in MV-4-11 xenografts .
Clinical Trial
Molecular Weight

502.60

Formula

C29H34N4O4
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(NC1=NOC(C(C)(C)C)=C1)NC2=CC=C(C#CC3=CC=C(OCCCN4CCOCC4)C=C3)C=C2
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 : 25 mg/mL (49.74 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 1.9897 mL 9.9483 mL 19.8965 mL
5 mM 0.3979 mL 1.9897 mL 3.9793 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)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

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.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9897 mL 9.9483 mL 19.8965 mL 49.7413 mL
5 mM 0.3979 mL 1.9897 mL 3.9793 mL 9.9483 mL
10 mM 0.1990 mL 0.9948 mL 1.9897 mL 4.9741 mL
15 mM 0.1326 mL 0.6632 mL 1.3264 mL 3.3161 mL
20 mM 0.0995 mL 0.4974 mL 0.9948 mL 2.4871 mL
25 mM 0.0796 mL 0.3979 mL 0.7959 mL 1.9897 mL
30 mM 0.0663 mL 0.3316 mL 0.6632 mL 1.6580 mL
40 mM 0.0497 mL 0.2487 mL 0.4974 mL 1.2435 mL
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

Clifutinib 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:

Clifutinib1862226-99-0FLT3ApoptosisRasp38 MAPKPI3KAktJAKSTATCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3Phosphoinositide 3-kinasePKBProtein kinase BJanus kinaseorally activeFLT3-ITDRAS/MAPKacute myeloid leukemiaInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Clifutinib
Cat. No.:
HY-172581
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

English - EN (251 KB) Français - FR (251 KB) Deutsch - DE (251 KB) Norwegian - NO (251 KB) Español - ES (251 KB) Swedish - SV (251 KB) Italian - IT (251 KB) Portuguese - PT (251 KB)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.