Powder: -20°C for 3 years | In solvent: -80°C for 1 year
(E/Z)-Zotiraciclib ((E/Z)-TG02) inhibits CDK2, JAK2, and FLT3 effectively with IC50s of 13, 73, and 56 nM, respectively.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 38.00 | |
2 mg | In stock | $ 54.00 | |
5 mg | In stock | $ 89.00 | |
10 mg | In stock | $ 122.00 | |
25 mg | In stock | $ 222.00 | |
50 mg | In stock | $ 367.00 | |
100 mg | In stock | $ 533.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 97.00 |
Description | (E/Z)-Zotiraciclib ((E/Z)-TG02) inhibits CDK2, JAK2, and FLT3 effectively with IC50s of 13, 73, and 56 nM, respectively. |
Targets&IC50 | JAK2:73 nM, FLT3:56 nM, CDK2:13 nM |
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]. |
Synonyms | (E/Z)-TG02, (E/Z)-SB1317 |
Molecular Weight | 372.46 |
Formula | C23H24N4O |
CAS No. | 937270-47-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 40mg/mL (107.39mM)
You can also refer to dose conversion for different animals. More
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(E/Z)-Zotiraciclib 937270-47-8 Angiogenesis Cell Cycle/Checkpoint Chromatin/Epigenetic JAK/STAT signaling Stem Cells Tyrosine Kinase/Adaptors FLT JAK CDK multiple myeloma JAK2 Fms like tyrosine kinase 3 (E/Z)-TG02 Cyclin dependent kinase (E/Z)-SB1317 FLT3 (E/Z)-SB 1317 Janus kinase CD135 leukemias Inhibitor (E/Z)-SB-1317 CDK2 Cluster of differentiation antigen 135 inhibit cancer (E/Z) Zotiraciclib (E/Z)Zotiraciclib inhibitor