bs-6621C

DATASHEET

Formulation Powder

Storage: Store in dry, dark place at -20C for 1 year.

Product Information:

Molecular Weight: 428.97

Formula: C23 H25 Cl N2 O2 S

CAS Number: 1338545-07-5

InChi Key: YHPWOYBWUWSJDW-UQKRIMTDSA-N

InChi: InChI=1S/C23H24N2O2S.ClH/c1-13-11-18(26)19(16-7-5-15(6-8-16)14(2)12-25(3)4)20-17-9-10-28-22(17)23(27)24-21(13)20;/h5-11,14,26H,12H2,1-4H3,(H,24,27);1H/t14-;/m0./s1

Smiles: Cl.CC1=CC(O)=C(C2=C1NC(=O)C1SC=CC=12)C1C=CC(=CC=1)[C@@H](C)CN(C)C

Purity: 98.0

Solubility: Soluble in DMSO, not in water

Appearance: Solid Power

Shelf Life: 1.0 years

Description:

OTS964 hydrochloride is a potent and selective TOPK inhibitor with potential anticancer activity. OTS964 inhibits TOPK kinase activity with high affinity and selectivity. Similar to the knockdown effect of TOPK small interfering RNAs (siRNAs), this inhibitor causes a cytokinesis defect and the subsequent apoptosis of cancer cells in vitro as well as in xenograft models of human lung cancer. Although administration of the free compound induced hematopoietic adverse reactions (leukocytopenia associated with thrombocytosis), the drug delivered in a liposomal formulation effectively caused complete regression of transplanted tumors without showing any adverse reactions in mice. ( Sci Transl Med. 2014 Oct 22;6(259):259ra145. )