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BOC Sciences |
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InvivoChem |
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+1-708-310-1919 +1-13798911105 |
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InvivoChem |
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OTS964 manufacturers
- OTS964
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- $1520.00
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2026-07-27
- CAS:1338542-14-5
- Purity:
- Supply Ability: 10g
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| Product Name: | OTS964 | | Synonyms: | Thieno[2,3-c]quinolin-4(5H)-one, 9-[4-[(1R)-2-(dimethylamino)-1-methylethyl]phenyl]-8-hydroxy-6-methyl-;OTS964(free base) | | CAS: | 1338542-14-5 | | MF: | C23H24N2O2S | | MW: | 392.51 | | EINECS: | | | Product Categories: | | | Mol File: | 1338542-14-5.mol |  |
| | OTS964 Chemical Properties |
| Boiling point | 501.7±50.0 °C(Predicted) | | density | 1.232±0.06 g/cm3(Predicted) | | pka | 9.46±0.20(Predicted) |
| | OTS964 Usage And Synthesis |
| Uses | OTS964 is an orally active, high affinity and selective TOPK inhibitor with an IC50 of 28 nM[1]. OTS964 is also a potent inhibitor of the cyclin-dependent kinase CDK11, which binds to CDK11B with a Kd of 40 nM[2]. | | in vivo | OTS964 (intravenously; 40 mg/kg on days 1, 4, 8, 11, 15, and 18) makes tumors shrinking even after the treatment and finally revealing complete regression[1].
OTS964 (oral administration; 50 or 100 mg/kg/day for 2 weeks) achieves complete tumor regression[1]. | Animal Model: | Nude mice bearing LU-99 lung cancer cells[1] | | Dosage: | 40 mg/kg | | Administration: | Intravenously; on days 1, 4, 8, 11, 15, and 18 | | Result: | The tumors continued shrinking even after the treatment and finally revealed complete regression.
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| Animal Model: | Nude mice bearing LU-99 lung cancer cells[1] | | Dosage: | 50 or 100 mg/kg | | Administration: |
Oral administration; once every day for 2 weeks | | Result: | Achieved complete tumor regression.
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| | IC 50 | TOPK: 28 nM (IC50); CDK11B: 40 nM (Kd) | | References | [1] Matsuo Y , et al. TOPK inhibitor induces complete tumor regression in xenograft models of human cancerthrough inhibition of cytokinesis. Sci Transl Med. 2014 Oct 22;6(259):259ra145. DOI:10.1126/scitranslmed.3010277
[2] Lin A, et al. Off-target toxicity is a common mechanism of action of cancer drugs undergoing clinical trials. Sci Transl Med. 2019 Sep 11;11(509). DOI:10.1126/scitranslmed.aaw8412
[3] Lu H, et al. TOPK inhibits autophagy by phosphorylating ULK1 and promotes glioma resistance to TMZ. Cell Death Dis. 2019 Aug 5;10(8):583. DOI:10.1038/s41419-019-1805-9 |
| | OTS964 Preparation Products And Raw materials |
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