TB22
TB22 is a non-nucleoside inhibitor of DOT1LR231Q, possessing anticancer activity. TB22 inhibits the malignant phenotype of lung cancer cells carrying the R231Q mutation through the MAPK/ERK signaling pathway, and can be used for lung cancer research.
For research use only. We do not sell to patients.
- Formula: C32H46ClN7O3S
- Molecular Weight:644.27
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Histone Methyltransferase Isoforms
More
Biological Activity
Description
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| NCI-H460 | IC50 |
19.97 μM
Compound: TB22
|
Antiproliferative activity against human NCI-H460 cells harboring wildtype DOT1L (unknown origin) (1 to 416 residues) assessed as inhibition of cell proliferation incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human NCI-H460 cells harboring wildtype DOT1L (unknown origin) (1 to 416 residues) assessed as inhibition of cell proliferation incubated for 72 hrs by CCK-8 assay
|
[PMID: 39255403] |
| NCI-H460 | IC50 |
2.85 μM
Compound: TB22
|
Antiproliferative activity against human NCI-H460 cells harboring DOT1L R231Q mutant (unknown origin) (1 to 416 residues) assessed as inhibition of cell proliferation incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human NCI-H460 cells harboring DOT1L R231Q mutant (unknown origin) (1 to 416 residues) assessed as inhibition of cell proliferation incubated for 72 hrs by CCK-8 assay
|
[PMID: 39255403] |
Chemical Information
-
Molecular Weight 644.27
-
Formula C32H46ClN7O3S
-
SMILES
CC(C1=CC=C(C=C1)NC(NCCCN(CCCN2CCOCC2)CC3(O)CN(CC3)C4=NC(Cl)=NC5=C4C=CS5)=O)(C)C
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
-
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)