SB1317 hydrochloride (1204918-72-8(free base)) (TG-02 hydrochloride) is an effective inhibitor of CDK2/JAK2/FLT3 (IC50: 13/73/56 nM).

FLT3:56 nM, JAK2:73nM, CDK2:13nM

SB1317 (25 μM) has no inhibition of Human CYP1A2, 3A4, 2C9, and 2C19 isoforms, but has inhibition of CYP2D6 (IC50: 0.95 μM). SB1317 inhibits cell proliferation of HCT-116 (IC50: 0.079 μM) and HL-60 (IC50: 0.059 μM)[1]. SB1317 is mainly metabolized by CYP3A4 and CY1A2 in vitro. SB1317 does not inhibit any of the major human CYPs in vitro except CYP2D6 (IC50=1 μM). CYP1A and CYP3A4 are mainly expressed in human hepatocytes in vitro.

SB1317 (75 mg/kg/day, p.o., 3×/week) markedly inhibits the growth of tumors with a mean TGI of 82%, while the lower dose (50 mg/kg/day, p.o., 3×/week) is marginally effective. Treatment with SB1317 using either regime significantly inhibits the growth of tumors with mean TGIs of 42% (p.o.) and 63% (i.p.), respectively[1]. In pharmacokinetic studies, SB1317 shows moderate to high systemic clearance (relative to liver blood flow), high volume of distribution (>0.6 L/kg), oral bioavailability of 24%, ~4 and 37% in mice, rats, and dogs, respectively; and extensive tissue distribution in mice.