| Name | SB1317 hydrochloride (1204918-72-8(free base)) |
| Description | SB1317 hydrochloride (1204918-72-8(free base)) (TG-02 hydrochloride) is an effective inhibitor of CDK2/JAK2/FLT3 (IC50: 13/73/56 nM). |
| In vitro | 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. |
| In vivo | 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. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 60 mg/mL (146.73 mM), Sonication is recommended.
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| Keywords | TG-02 Hydrochloride | TG02 Hydrochloride | TG 02 Hydrochloride | SB1317 hydrochloride (1204918-72-8(free base)) | SB-1317 hydrochloride (1204918-72-8(free base)) | SB1317 hydrochloride (1204918728(free base)) | SB1317 hydrochloride (1204918 72 8(free base)) | JAK2 | FLT3 | CDK2 |
| Inhibitors Related | Ribociclib | Gilteritinib | Nintedanib | Sorafenib | Tofacitinib Citrate | Abemaciclib | Pexidartinib | Sorafenib tosylate | Ruxolitinib phosphate | CASIN | Dinaciclib | Abemaciclib methanesulfonate |
| Related Compound Libraries | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Kinase Inhibitor Library | Tyrosine Kinase Inhibitor Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Immunology/Inflammation Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Anti-Cancer Drug Library | Anti-Cancer Active Compound Library |
United States
