Cat. No.: HY-172581

Clifutinib

고객리뷰

Based on 1 Customer Validation

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.

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

Purity: 99.59%
CAS No.: 1862226-99-0
화학식: C₂₉H₃₄N₄O₄
분자량:502.60

보관:

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

Clifutinib Chemical Structure

CAS No.: 1862226-99-0

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biological Activity
- 제품 설명
- In Vitro
- Parmacokinetics
- In Vivo
- Clinical Trial
Chemical Information
용액&용해도
- In Vitro
순도&문서
References
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

All Ras Isoforms :

All p38 MAPK Isoforms :

All PI3K Isoforms :

All Akt Isoforms :

All JAK Isoforms :

All STAT Isoforms :

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 No. 1862226-99-0
Appearance Solid
분자량 502.60
화학식 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
선적

Room temperature in continental US; may vary elsewhere.

보관

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

용액&용해도

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.

몰농도 계산기

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

순도&문서

Select Batch:

Purity: 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)

References

[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

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All Ras Isoforms

All p38 MAPK Isoforms

All PI3K Isoforms

All Akt Isoforms

All JAK Isoforms

All STAT Isoforms

Biological Activity

Chemical Information

용액&용해도

순도&문서

References

Help & FAQs