化合物SB1317 hydrochloride T4227

Product Introduction
Bioactivity


英文名: SB1317 hydrochloride (1204918-72-8(free base))

描述: SB1317 hydrochloride (1204918-72-8(free base)) (TG-02 hydrochloride) 是一种有效的 CDK2/JAK2/FLT3 抑制剂（IC50：13/73/56 nM）。

体外活性: 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.

体内活性: 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.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 26.5 mg/mL


关键字: TG02 Hydrochloride | SB1317 hydrochloride (1204918-72-8(free base)) | SB1317 hydrochloride (1204918 72 8(free base)) | SB-1317 hydrochloride (1204918-72-8(free base)) | SB1317 hydrochloride (1204918728(free base)) | TG-02 Hydrochloride | TG 02 Hydrochloride

相关产品: Allitinib tosylate | Edicotinib | Crenolanib | FLT3-IN-10 | UNC2541 | Quizartinib | AZD2932 | Onatasertib | CHMFL-FLT3-122 | BMS-2

相关库: JAK-STAT Compound Library | Drug Repurposing Compound Library | Anti-Cancer Drug Library | Anti-Lung Cancer Compound Library | Anti-Cancer Clinical Compound Library | Kinase Inhibitor Library | Inhibitor Library | Anti-Cancer Active Compound Library | Tyrosine Kinase Inhibitor Library | Stem Cell Differentiation Compound Library

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