SB-743921

SB-743921 is a potent, selective kinesin spindle protein (KSP) inhibitor with Ki of 0.1 nM, shows no activity against MKLP1, Kin2, Kif1A, Kif15, KHC, Kif4 and CENP-E; also shows high affinity for mouse KSP with Ki of 0.12 nM; blocks assembly of a functional mitotic spindle, thereby causing cell cycle arrest in mitosis and subsequent cell death in cancer cells, demonstrates improved potency over ispinesib in both biochemical and cellular assays; shows a broad spectrum of tumor inhibition in multiple cancer models.Blood Cancer Phase 2 Discontinued (In Vitro) :SB-743921 is a potent inhibitor of Eg5, with a Ki of 0.1 nM. SB-743921 (1 nM) potently inhibits colony forming cell (CFC) formation of chronic myeloid leukemia (CML) primary cells, but exhibits slight inhibitory activities on the colony-forming ability of normal bone marrow progenitors. SB-743921 (1, 3 nM) induces apoptosis of CML primary CD34 + cells, and shows slight effect on normal CD34 + cells. SB-743921 (2 nM) in combination with imatinib displays additive anti-proliferative effect in KCL22 and CML CD34 + cells. Furthermore, SB-743921 overcomes imatinib resistance in CML cells. SB-743921 (0.5 nM, 1 nM, 3 nM) inhibits MEK/ERK and AKT signaling in CML cells. (In Vivo) :SB-743921 has good oral bioavailability and pharmacokinetics and induces complete tumor regression in nude mice bearing lung cancer patient xenografts.

940929-33-9

SB743921 | SB 743921

>98% (HPLC)

10 mM in DMSO

CC1=CC=C (C=C1) C (=O) N (CCCN) C (C2=C (C (=O) C3=C (O2) C=C (C=C3) Cl) CC4=CC=CC=C4) C (C) C.Cl

C31H34Cl2N2O3

553.5193

Storage temperature: -20°C. Stability: ≥ 2 years

For research use only.