HP1142
HP1142 is a potent and selective inhibitor of FLT3 receptor tyrosine kinase (FLT3/ITD mutation). HP1142 is a benzoimidazole scaffold-based compound. HP1142 has the potential for the research of FLT3/ITD leukemia.
For research use only. We do not sell to patients.
- CAS No.: 381173-58-6
- Formula: C22H21N3O2
- Molecular Weight:359.42
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| BaF3 | IC50 |
>0.4 μM
Compound: HP1142
|
Antiproliferative activity against mouse BaF3 cells expressing wild type FLT3 assessed as reduction in cell viability measured after 72 hrs by MTS assay
Antiproliferative activity against mouse BaF3 cells expressing wild type FLT3 assessed as reduction in cell viability measured after 72 hrs by MTS assay
|
[PMID: 35148084] |
| HL-60 | IC50 |
>50 μM
Compound: HP1142
|
Antiproliferative activity against human HL-60 cells expressing wild type FLT3 assessed as reduction in cell viability measured after 72 hrs by MTS assay
Antiproliferative activity against human HL-60 cells expressing wild type FLT3 assessed as reduction in cell viability measured after 72 hrs by MTS assay
|
[PMID: 35148084] |
| MOLM-13 | IC50 |
113.4 nM
Compound: HP1142
|
Antiproliferative activity against human MOLM-13 cells harboring FLT3-ITD mutant assessed as reduction in cell viability measured after 72 hrs by MTS assay
Antiproliferative activity against human MOLM-13 cells harboring FLT3-ITD mutant assessed as reduction in cell viability measured after 72 hrs by MTS assay
|
[PMID: 35148084] |
| MV4-11 | IC50 |
189 nM
Compound: HP1142
|
Antiproliferative activity against human MV4-11 cells harboring FLT3-ITD mutant assessed as reduction in cell viability measured after 72 hrs ny MTS assay
Antiproliferative activity against human MV4-11 cells harboring FLT3-ITD mutant assessed as reduction in cell viability measured after 72 hrs ny MTS assay
|
[PMID: 35148084] |
Chemical Information
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CAS No. 381173-58-6
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Molecular Weight 359.42
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Formula C22H21N3O2
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SMILES
COC(C(OC)=C1)=CC=C1CNC2=CC3=C(C=C2)N(C4=CC=CC=C4)C=N3
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Genotoxicity/Mutagenicity Study
The bacterial reverse mutation assay detects point mutations that restore amino-acid prototrophy in auxotrophic Salmonella typhimurium or Escherichia coli tester strains; after exposure to a test article, mutagenic activity is read out as an increased number of revertant colonies on minimal agar compared with the vehicle control. The assay uses tester strains with different mutation targets so that base-substitution and frameshift mutagens can be detected, and testing is performed with and without exogenous mammalian metabolic activation because some chemicals require biotransformation to become mutagenic.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)