Referencia número: 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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Pureza: 99.59%
No. CAS: 1862226-99-0
Fòrmula: C₂₉H₃₄N₄O₄
Peso molecular:502.60

Almacenamiento:

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

Clifutinib Chemical Structure

No. CAS: 1862226-99-0

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

Actividad biológica
- Descripciòn
- In Vitro
- Parmacokinetics
- In Vivo
- Ensayo clínico
Chemical Information
Solvente y solubilidad
- In Vitro
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

Ver todos los productos específicos de isoformas Ras :

Ver todos los productos específicos de isoformas p38 MAPK :

Ver todos los productos específicos de isoformas PI3K :

Ver todos los productos específicos de isoformas Akt :

Ver todos los productos específicos de isoformas JAK :

Ver todos los productos específicos de isoformas STAT :

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 .

Ensayo clínico

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

Chemical Information

No. CAS 1862226-99-0
Appearance Solid
Peso molecular 502.60
Fòrmula 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
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

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

Solvente y solubilidad

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.

Calculadora de molaridad

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (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)
Instrucciones de manejo (2659 KB)

Referencias

[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

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Ver todos los productos específicos de isoformas Ras

Ver todos los productos específicos de isoformas p38 MAPK

Ver todos los productos específicos de isoformas PI3K

Ver todos los productos específicos de isoformas Akt

Ver todos los productos específicos de isoformas JAK

Ver todos los productos específicos de isoformas STAT

Actividad biológica

Chemical Information

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs