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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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O650852-2mg | 2mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $115.90 | |
O650852-5mg | 5mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $205.90 | |
O650852-10mg | 10mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $340.90 | |
O650852-25mg | 25mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $646.90 | |
O650852-50mg | 50mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $1,033.90 | |
O650852-100mg | 100mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $1,650.90 |
Specifications & Purity | ≥98% |
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Biochemical and Physiological Mechanisms | OTS514 is a highly potent TOPK inhibitor with an IC 50 of 2.6 nM. OTS514 strongly suppresses the growth of TOPK-positive cancer cells. OTS514 induces cell cycle arrest and apoptosis. |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Product Description | OTS514 is a highly potent TOPK inhibitor with an IC 50 of 2.6 nM. OTS514 strongly suppresses the growth of TOPK-positive cancer cells OTS514 induces cell cycle arrest and apoptosis . In Vitro OTS514 (1.5625-100 nM) induces cell cycle arrest and apoptosis at nanomolar concentrations in a series of human myeloma cell lines (HMCL) and prevents outgrowth of a putative CD138 + stem cell population from multiple myeloma (MM) patient-derived peripheral blood mononuclear cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: Human myeloma cell lines (MM1.S, MM1.R, RPMI 8226, 8226Dox40, KMS34, KMS34CFZ, KMS11, JJN3, LP-1, NCI H929, U266B1) Concentration: 1.5625, 3.125, 6.25, 12.5, 25, 50, and 100 nM Incubation Time: 72 hours Result: IC 50 values ranged from 11.6 to 29.4 nM in parental cell lines, indicating a potent inhibitory effect. Only the RPMI 8226-Dox40 cell line, which overexpresses the multi-drug resistance transporter gene ABCB1, is resistant. In Vivo OTS514 (1-5 mg/kg; once a day for 2 weeks; intravenous administration) induces tumor regression in a xenograft model of A549 cells (TOPK-positive lung cancer cells) . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Female BALB/cSLC-nu/nu mice bearing a xenograft model of A549 cells Dosage: 1, 2.5, and 5 mg/kg Administration: Intravenously treated; once every day for 2 weeks Result: Resulted in tumor growth inhibition (TGI) of 5.7, 43.3, and 65.3% on day 15, respectively, without any body weight loss. Form:Solid IC50& Target:IC50: 2.6 nM (TOPK) |
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Mechanism of Action | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | References |
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IUPAC Name | 9-[4-[(2R)-1-aminopropan-2-yl]phenyl]-8-hydroxy-6-methyl-5H-thieno[2,3-c]quinolin-4-one |
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INCHI | InChI=1S/C21H20N2O2S/c1-11-9-16(24)17(14-5-3-13(4-6-14)12(2)10-22)18-15-7-8-26-20(15)21(25)23-19(11)18/h3-9,12,24H,10,22H2,1-2H3,(H,23,25)/t12-/m0/s1 |
InChi Key | OETLNMOJNONWOY-LBPRGKRZSA-N |
Canonical SMILES | CC1=CC(=C(C2=C1NC(=O)C3=C2C=CS3)C4=CC=C(C=C4)C(C)CN)O |
Isomeric SMILES | CC1=CC(=C(C2=C1NC(=O)C3=C2C=CS3)C4=CC=C(C=C4)[C@@H](C)CN)O |
PubChem CID | 67448836 |
Molecular Weight | 364.46 |
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Solubility | DMSO : 100 mg/mL (274.38 mM; Need ultrasonic) |
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