[CAS NO. 1431697-89-0] OTSSP167
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PRODUCTS SPECIFICATIONS [1431697-89-0]
Distributor
Catalog
SLK-S7159
Brand
Selleck
CAS
1431697-89-0
DESCRIPTION [1431697-89-0]
Overview
| MDL | MFCD23160047 |
|---|---|
| Molecular Weight | 487.42 |
| Molecular Formula | C25H28Cl2N4O2 |
| SMILES | CC(C1=C(N[C@H]2CC[C@H](CN(C)C)CC2)C3=NC(C4=CC(Cl)=C(O)C(Cl)=C4)=CC=C3N=C1)=O |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0516 mL | 10.2581 mL | 20.5162 mL |
| 5 mM | 0.4103 mL | 2.0516 mL | 4.1032 mL |
| 10 mM | 0.2052 mL | 1.0258 mL | 2.0516 mL |
| 50 mM | - | - | - |
Description
OTSSP167 (OTS167) is a highly potent (maternal embryonic leucine zipper kinase) inhibitor with of 0.41 nM.
Features
MELK-selective inhibitor.
Targets
| MELK [1] (Cell-free assay) |
| 0.41 nM |
In vitro
OTSSP167 inhibits A549, T47D, DU4475, and 22Rv1 cancer cells, in which MELK is highly expressed, with IC50 values of 6.7, 4.3, 2.3, and 6.0 nM, respectively. OTSSP167 inhibited the phosphorylation of PSMA1 (proteasome subunit alpha type 1) and DBNL (drebrin-like), which are novel MELK substrates and are important for stem-cell characteristics and invasiveness. OTSSP167 suppresses mammosphere formation of breast cancer cells through the inhibition of PSMA1 phosphorylation.
In vivo
OTSSP167 exhibits significant tumor growth suppression in xenograft studies using breast, lung, prostate, and pancreas cancer cell lines in mice by both intravenous and oral administration. In MDA-MB-231 model, intravenous administration of OTSSP167 at 20 mg/kg once every two days results in TGI of 73% The oral administration at 10 mg/kg once a day reveals TGI of 72%. OTSSP167 for multiple cancer types in dose-dependent and MELK-dependent manners with no or a little body-weight loss.
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