K 03861is a potent and selective Type II FLT3 inhibitor. K 03861 is able to override drug resistance that less potent "type I" inhibitors and "type II" first-generation FLT3 inhibitors cannot. Constitutively activated mutant FLT3 has emerged as a promising target for therapy for the subpopulation of acute myeloid leukemia (AML) patients who harbor it. The small molecule inhibitor, PKC412, targets mutant FLT3 and is currently in late-stage clinical trials. However, the identification of PKC412-resistant leukemic blast cells in the bone marrow of AML patients has propelled the development of novel and structurally distinct FLT3 inhibitors that have the potential to override drug resistance and more efficiently prevent disease progression or recurrence.
CAS Number: 853299-07-7
Molecular Weight: 501.50
Chemical Name: 1-(4-((2-aminopyrimidin-4-yl)oxy)phenyl)-3-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)urea
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: Soluble in DMSO, not in water
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
K 03861(AUZ-454) (10-20 μM; 1, 2, 3, and 4 days) has a inhibitory effect on Caki-1 and ACHN cells with WTAP overexpression by CCK8 assays. K 03861(AUZ-454) (10 μM; 24 hours) decreases the colony fold in Caki-1 and ACHN cells through a CDK2-dependent mechanism.
- Weisberg E, Roesel J, Furet P, Bold G, Imbach P, FlÃ¶rsheimer A, Caravatti G, Jiang J, Manley P, Ray A, Griffin JD. Antileukemic Effects of Novel First- and Second-Generation FLT3 Inhibitors: Structure-Affinity Comparison. Genes Cancer. 2010 Oct;1(10):1021-32. doi: 10.1177/1947601910396505. PubMed PMID: 21779428; PubMed Central PMCID: PMC3092267.
Products are for research use only. Not for human use.
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