Clifutinib free base

Clifutinib is an orally active and selective internal tandem duplication mutation of FMS-like tyrosine kinase 3 inhibitor.

For research use only. Not for human or veterinary use.

Target FLT3 Apoptosis Ras p38 MAPK PI3K Akt JAK STAT

Research area Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

Clifutinib structure

CAS No.: 1862226-99-0

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Pack sizes & pricing

Size	Price	SKU	Stock
50 mg	USD 450.00	BP-01938-50mg	In stock	Get quote
100 mg	USD 650.00	BP-01938-100mg	In stock	Get quote
250 mg	USD 1,150.00	BP-01938-250mg	In stock	Get quote
500 mg	USD 1,750.00	BP-01938-500mg	In stock	Get quote
1 g	Inquire	BP-01938-1g	Inquire	Inquire

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Description

Clifutinib (Compound 9e) 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 inhibits the activity of FLT3-ITD kinase and blocks the downstream RAS/MAPK, PI3K/AKT, and JAK/STAT5 signaling pathways of FLT3. Clifutinib is promising for research of relapsed/refractory FLT3-ITD-positive acute myeloid leukemia.

Biological activity

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. Clifutinib (9e, 0.1-1000 nM, 72 h) exhibits potent antiproliferative activity against Ba/F3 cells expressing FLT3 mutant isoforms, while showing no antiproliferative effect on parental Ba/F3 cells with IC50 > 1000 nM. Clifutinib (1-100 nM, 48-72 h) induces apoptosis in MV-4-11 cells in a dose-dependent manner. 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. 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.

Identifiers

SMILES: O=C(NC1=NOC(=C1)C(C)(C)C)NC2=CC=C(C#CC3=CC=C(OCCCN4CCOCC4)C=C3)C=C2
InChIKey: DWZXYPARIPYQKS-UHFFFAOYSA-N

Specifications

MW (average): 502.6047
Formula: C₂₉H₃₄N₄O₄
CAS No.: 1862226-99-0
Physical state: Solid
Color: white to off-white
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder 4℃, sealed storage, 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO

Documents

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.

Same target

Search FLT3

Same research area

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