AC220

Inhibitor of FLT3

Structure

Information

Protein target names: FLT3

Mechanism of action: Inhibitor

Recommended in-cell concentration:
1 nM - 300 nM

In Vitro Validations

Uniprot ID: P36888
Target Class: Kinase
Target SubClass: TK
Potency: KD
Potency Value: 1.6 nM
Potency Assay: In vitro binding assay
PDB ID for probe-target interaction (3D structure): --
Target aliases:
Receptor-type tyrosine-protein kinase FLT3, STK1, ...

DOI Reference: 10.1182/blood-2009-05-222034

In Cell Validations

In Vivo Data

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SERP ratings and comments


SERP Ratings

In Cell Rating

Comments:

This probe has a number of targets other than FLT3 and is active at 300 nM in human primary cell assays that do not express FLT3. If used as a target-selective probe in a study, this data should be supplemented by target knock-down and over expression of a constitutively active form to confirm involvement of the target.

(last updated: 22 May 2016 )

SERP Ratings

In Cell Rating
In Model Organisms

Comments:

AC220 is potent and selective and has good PK characteristics. While activity in certain biochemical assays and cellular assays may be evident as low as 0.1-10 nM, drug-resistant models may require concentrations as high as 100-300 nM. It has been compared with and/or combined with other anticancer agents such as G-749 (FLT3 inhibitor) and JQ1 (BET protein antagonist) in various models, with resistant AML being an initial disease target in humans.

(last updated: 23 May 2016 )

SERP Ratings

In Cell Rating
In Model Organisms

Comments:

No nonhuman ortholog potencies were reported. Acute oral dosing in mice was shown be tolerated (up to 300 mg/kg), though PK was linear up through 100 mg/kg. Repeat dosing was only performed at 10 mg/kg. RET, PDGFRA, PDGFRB, CSF1R are the only kinases within 10x. The recommended upper in vitro concentration is intended to minimize off-target RTK activity.

(last updated: 23 May 2016 )