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PTC-596

Chemical Structure : PTC-596

CAS No.: 1610964-64-1

PTC-596 (Unesbulin, PTC 596, PTC596)

Catalog No.: PC-60486Not For Human Use, Lab Use Only.

PTC-596 (Unesbulin, PTC596) is a novel, orally active, small molecule inhibitor of BMI-1 that accelerates BMI-1 degradation, inhibits AML cells growth with IC50 of <100 nM.

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Purity & Documentation Purity: 98.65% Select Batch:

Biological Activity

PTC-596 (Unesbulin, PTC596) is a novel, orally active, small molecule inhibitor of BMI-1 that accelerates BMI-1 degradation, inhibits AML cells growth with IC50 of <100 nM.
PTC-596 is a direct microtubule polymerization inhibitor.
PTC-596 reduces total BMI-1 protein levels by 87% and 61% in MOLM-13 and OCI-AML3 cells at 100 nM, induces apoptosis and reduces the levels of ubiquitylated histone H2A.
PTC-596 downregulates MCL-1 and induces p53-independent mitochondrial apoptosis in acute myeloid leukemia progenitor cells.

Physicochemical Properties

M.Wt 420.347
Formula C19H13F5N6
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

5-fluoro-2-(6-fluoro-2-methyl-1H-benzo[d]imidazol-1-yl)-N4-(4-(trifluoromethyl)phenyl)pyrimidine-4,6-diamine

References

1. Nishida Y, et al. Blood Cancer J. 2017 Feb 17;7(2):e527.

2, Eberle-Singh JA, et al. Clin Cancer Res. 2019 Jun 7. pii: clincanres.3281.2018. doi: 10.1158/1078-0432.CCR-18-3281.

3, Maeda A, et al. Oncotarget. 2018 Jun 19;9(47):28547-28560.

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