OTS964 free base · Synonyms: OTS-964 · OTS 964

OTS964 hydrochloride is an orally active, high affinity and selective TOPK inhibitor.

For research use only. Not for human or veterinary use.

Target TOPK CDK Apoptosis

Research area Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

OTS964 structure

CAS No.: 1338545-07-5

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
500 mg	USD 472.00	BP-02492-500mg	In stock	Get quote
1 g	USD 755.00	BP-02492-1g	In stock	Get quote
2 g	USD 1,200.00	BP-02492-2g	In stock	Get quote
3 g	USD 1,450.00	BP-02492-3g	In stock	Get quote
5 g	USD 1,930.00	BP-02492-5g	In stock	Get quote
10 g	USD 3,090.00	BP-02492-10g	In stock	Get quote

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Description

OTS964 hydrochloride is an orally active, high affinity and selective TOPK (T-lymphokine-activated killer cell-originated protein kinase) inhibitor with an IC50 of 28 nM . OTS964 hydrochloride is also a potent inhibitor of the cyclin-dependent kinase CDK11, which binds to CDK11B with a Kd of 40 nM .

Biological activity

In Vitro OTS964 hydrochloride (10 nM; 48 hours) suppresses cancer cell proliferation. OTS964 hydrochloride (10 nM; 48 hours) increases cancer cell death. OTS964 (0.1-2 μM; 24 and 48 hours) increases the expression of LC3-II and decreases the expression of P62, both in a dose-dependent manner. In Vivo OTS964 hydrochloride (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. OTS964 hydrochloride (oral administration; 50 or 100 mg/kg/day for 2 weeks) ultimately achieves complete tumor regression.

Identifiers

SMILES: Cl.C[C@@H](CN(C)C)C1=CC=C(C=C1)C1=C(O)C=C(C)C2=C1C1=C(SC=C1)C(=O)N2
InChIKey: YHPWOYBWUWSJDW-UQKRIMTDSA-N

Specifications

MW (average): 428.9750
Formula: C₂₃H₂₅ClN₂O₂S
CAS No.: 1338545-07-5
Physical state: Solid
Color: Off-white to light yellow
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder 4°C, sealed storage, away from moisture; In solvent -20°C, 1 year;

Solubility

Soluble in DMSO/H2O

Documents

References

[1]. Matsuo Y, et al. TOPK inhibitor induces complete tumor regression in xenograft models of human cancer through inhibition ofcytokinesis. Sci Transl Med. 2014 Oct 22;6(259):259ra145.

[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).

[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.

Same target

Search TOPK

Same research area

Search Cancer