| Name | (E/Z)-Zotiraciclib |
| Description | (E/Z)-Zotiraciclib ((E/Z)-TG02) effectively inhibits CDK2, JAK2, and FLT3 with IC50s of 13 nM, 73 nM, and 56 nM, respectively. |
| In vitro | (E/Z)-Zotiraciclib has a highly novel kinase inhibitory spectrum inhibiting 17 kinases from a panel of 63, 11 of which are CDK/JAK/FLT family members. Human CYP1A2, 3A4, 2C9, and 2C19 isoforms are not inhibited by (E/Z)-Zotiraciclib at the highest tested concentration of 25 μM, but (E/Z)-Zotiraciclib inhibits CYP2D6 with an IC50 of 0.95 μM, approximately at the plasma Cmax?observed at the maximum tolerated dose. (E/Z)-Zotiraciclib inhibits cell proliferation concentrations in HCT-116 with an IC50 of 0.079 μM and HL-60 with an IC50 of 0.059 μM[1]. (E/Z)-Zotiraciclib is a novel small molecule potent CDK/JAK2/FLT3 inhibitor and mainly metabolized by CYP3A4 and CY1A2 in vitro[2]. |
| In vivo | Treatment with (E/Z)-Zotiraciclib (75 mg/kg p.o. q.d. 3×/week) significantly inhibits the growth of tumors with a mean TGI of 82%, while the lower dose(50 mg/kg p.o. 3×/week) is marginally effective. Treatment with (E/Z)-Zotiraciclib using either regime significantly inhibits the growth of tumors with mean TGIs of 42% and 63% for the oral and ip delivery methods, respectively[1]. In pharmacokinetic studies, (E/Z)-Zotiraciclib shows moderate to high systemic clearance (relative to liver blood flow), high volume of distribution (>0.6 L/kg), the oral bioavailability of 24%, ~4 and 37% in mice, rats, and dogs, respectively; and extensive tissue distribution in mice[2]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween-80+45% Saline : 1 mg/mL (2.68 mM), Sonication is recommended.
DMSO : 20 mg/mL (53.7 mM), Sonication is recommended.
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| Keywords | multiple myeloma | leukemias | Janus kinase | JAK2 | JAK | Inhibitor | inhibit | Fms like tyrosine kinase 3 | FLT3 | Cyclin dependent kinase | Cluster of differentiation antigen 135 | CDK2 | CDK | CD135 | cancer | (E/Z)-Zotiraciclib | (E/Z)Zotiraciclib | (E/Z)-SB-1317 | (E/Z)-SB 1317 | (E/Z) Zotiraciclib |
| Inhibitors Related | Ribociclib | Gilteritinib | 2-Chloropyrazine | Kojic acid | Ruxolitinib | Sorafenib | Abemaciclib | Resveratrol | Pexidartinib | 2,4,6-Trihydroxybenzoic acid | Palbociclib | Lentinan |
| 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
