Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C25H28Cl2N4O2 |
Molecular Weight | 487.421 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 2 / 2 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CN(C)C[C@H]1CC[C@@H](CC1)NC2=C(C=NC3=C2N=C(C=C3)C4=CC(Cl)=C(O)C(Cl)=C4)C(C)=O
InChI
InChIKey=DKZYXHCYPUVGAF-JCNLHEQBSA-N
InChI=1S/C25H28Cl2N4O2/c1-14(32)18-12-28-22-9-8-21(16-10-19(26)25(33)20(27)11-16)30-24(22)23(18)29-17-6-4-15(5-7-17)13-31(2)3/h8-12,15,17,33H,4-7,13H2,1-3H3,(H,28,29)/t15-,17-
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/27082996
Sources: https://www.ncbi.nlm.nih.gov/pubmed/27082996
OTS-167 is a maternal embryonic leucine zipper kinase (MELK) inhibitor which demonstrated antitumor properties in laboratory tests. It is being developed as an anti-cancer drug. The compound has been shown to suppress the growth of breast, lung, pancreatic and prostate cancer cells that express high levels of the MELK protein. OTS167 reached phase II clinical trials in patients with AML, ALL, advanced MDSs, advanced MPNs, or advanced CML and phase I in patients with breast cancer.
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
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Target ID: Q14680|||B7Z6Y0 Gene ID: 9833.0 Gene Symbol: MELK Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/24657156 |
0.41 nM [IC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
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Primary | Unknown Approved UseUnknown |
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Primary | Unknown Approved UseUnknown |
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Primary | Unknown Approved UseUnknown |
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Primary | Unknown Approved UseUnknown |
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Primary | Unknown Approved UseUnknown |
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Primary | Unknown Approved UseUnknown |
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Primary | Unknown Approved UseUnknown |
Sample Use Guides
In Vivo Use Guide
Sources: https://clinicaltrials.gov/ct2/show/NCT02768519
In phase I clinical trial on healthy participants OST-167 was given at doses 0.5 mg, 1.0 mg, and 2.0 mg .
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/27082996
HeLaM or MCF7 cell lines were treated with 100nM OTS-167 for 2 hours to test the effect of the drug on mitosis.
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NCI_THESAURUS |
C61074
Created by
admin on Sat Dec 16 10:17:41 GMT 2023 , Edited by admin on Sat Dec 16 10:17:41 GMT 2023
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1431697-89-0
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DTXSID90856134
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C111569
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OTS-167
Created by
admin on Sat Dec 16 10:17:41 GMT 2023 , Edited by admin on Sat Dec 16 10:17:41 GMT 2023
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PRIMARY | Description: Maternal embryonic leucine zipper kinase (MELK) is a serine/threonine kinase that regulates signaling central to cell cycling, stem cell renewal, apoptosis, and other cellular processes. MELK is overexpressed in some forms of cancer, particularly those with aggressive undifferentiated tumors. OTSSP167 is a potent inhibitor of MELK (IC50 = 0.41 nM). It suppresses the growth of diverse cancer cell lines at low nanomolar concentrations.5 It also blocks the phosphorylation of MELK-specific substrates and reduces the ability of MCF-7 breast cancer cells to invade and form spheroids in Matrigel.5 OTSSP167 is also effective in vivo when delivered either orally or intravenously, suppressing the growth of xenograft tumors in mice. | ||
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VY778IXU5T
Created by
admin on Sat Dec 16 10:17:41 GMT 2023 , Edited by admin on Sat Dec 16 10:17:41 GMT 2023
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ACTIVE MOIETY
SALT/SOLVATE (PARENT)