Art. -Nr.: HY-172581

Clifutinib

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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.

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Reinheit: 99.59%
CAS. Nr.: 1862226-99-0
Formel: C₂₉H₃₄N₄O₄
Molecular Weight:502.60

Speicherung:

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

Clifutinib Chemical Structure

CAS. Nr.: 1862226-99-0

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Use of MCE Products

Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- In Vitro
- Parmacokinetics
- In Vivo
- Clinical Trial
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Alle Ras Isoform-spezifische Produkte anzeigen :

Alle p38 MAPK Isoform-spezifische Produkte anzeigen :

Alle PI3K Isoform-spezifische Produkte anzeigen :

Alle Akt Isoform-spezifische Produkte anzeigen :

Alle JAK Isoform-spezifische Produkte anzeigen :

Alle STAT Isoform-spezifische Produkte anzeigen :

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.

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.

Parmacokinetics

Species	Dose	Route	T_max	C_max	AUC_last	T_1/2	CL	V_ss	F
Dog^[1]	1 mg/kg	i.v.	0.083 h	633 ng/mL	1290 ng·h/mL	6.28 h	11.3 mL/min/kg	5.08 L/kg	/
Dog^[1]	5 mg/kg	p.o.	1.67 h	520 ng/mL	4870 ng·h/mL	7.41 h	/	/	71.91 %
Mice^[1]	10 mg/kg	p.o.	0.5 h	1660 ng/mL	4380 ng·h/mL	1.73 h	/	/	50.3 %
Mice^[1]	2 mg/kg	i.v.	0.083 h	1820 ng/mL	1.740 ng·h/mL	1.17 h	18.9 mL/min/kg	1.36 L/kg	/
Monkey^[1]	1 mg/kg	i.v.	0.083 h	4720 ng/mL	10100 ng·h/mL	13.1 h	1.35 mL/min/kg	0.996 L/kg	/
Monkey^[1]	5 mg/kg	p.o.	4 h	1410 ng/mL	10800 ng·h/mL	8.94 h	/	/	20.05 %

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

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

Chemical Information

CAS. Nr. 1862226-99-0
Appearance Solid
Molecular Weight 502.60
Formel C₂₉H₃₄N₄O₄
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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Lösungsmittel & Löslichkeit

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)

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

1.9897 mL

9.9483 mL

19.8965 mL

5 mM

0.3979 mL

1.9897 mL

3.9793 mL

10 mM

0.1990 mL

0.9948 mL

1.9897 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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

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

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 KB)
SDS (251 KB)
- 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)
- Korean - KR (251 KB)
- Portuguese - PT (251 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]. Liu B, et al. Discovery of FLT3-ITD Inhibitor Clifutinib: A Novel Biphenylacetylene Urea Derivative in Clinical Trials for the Treatment of Relapsed/Refractory FLT3-ITD+ Acute Myeloid Leukemia. J Med Chem. 2025 Apr 24;68(8):7955-7972. [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	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

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Clifutinib

Apoptosis Compound Library

Epigenetics Compound Library

GPCR/G Protein Compound Library

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

Kinase Inhibitor Library

MAPK Compound Library

PI3K/Akt/mTOR Compound Library

Protein Tyrosine Kinase Compound Library

Stem Cell Signaling Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

Differentiation Inducing Compound Library

Reprogramming Compound Library

Oxygen Sensing Compound Library

Ferroptosis Compound Library

Glycolysis Compound Library

Pyroptosis Compound Library

Cytoskeleton Compound Library

Orally Active Compound Library

Glutamine Metabolism Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Neurodegenerative Disease-related Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Transcription Factor-Targeted Library

Glucose Metabolism Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Antidepressant Compound Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Cancer Stem Cells Compound Library

Pain-Related Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Autoimmune Disease Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cytokine Inhibitors Library

Cell Death Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Anti-Gastric Cancer Compound Library

Anti-Fibrosis Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Lactylation Compound Library

Alkyne Compound Library

Alle Ras Isoform-spezifische Produkte anzeigen

Alle p38 MAPK Isoform-spezifische Produkte anzeigen

Alle PI3K Isoform-spezifische Produkte anzeigen

Alle Akt Isoform-spezifische Produkte anzeigen

Alle JAK Isoform-spezifische Produkte anzeigen

Alle STAT Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs