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(E/Z)-Zotiraciclib

Catalog No. T21503 CAS 937270-47-8

Synonyms: (E/Z)-SB1317, (E/Z)-TG02

(E/Z)-Zotiraciclib inhibits <a href="/target/CDK" style="display: inline; color: #c13a36">CDK</a>2, <a href="/target/JAK" style="display: inline; color: #c13a36">JAK</a>2, and <a href="/target/FLT" style="display: inline; color: #c13a36">FLT</a>3 effectively with IC50s of 13, 73, and 56 nM, respectively.

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(E/Z)-Zotiraciclib, CAS 937270-47-8

Pack Size	Availability	Price/USD
2 mg	In stock	$ 66.00
5 mg	In stock	$ 99.00
10 mg	In stock	$ 139.00
25 mg	In stock	$ 257.00
50 mg	In stock	$ 399.00
100 mg	In stock	$ 588.00
200 mg	In stock	$ 878.00
1 mL * 10 mM (in DMSO)	In stock	$ 114.00

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Purity: 97.75%

Purity: 98%

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Description	(E/Z)-Zotiraciclib 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)-SB1317, (E/Z)-TG02
Molecular Weight	372.46
Formula	C23H24N4O
CAS No.	937270-47-8

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 40mg/mL (107.39mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. William AD, et al. Discovery of kinase spectrum selective macrocycle (16E)-14-methyl-20-oxa-5,7,14,26-tetraazatetracyclo[19.3.1.1(2,6).1(8,12)]heptacosa-1(25),2(26),3,5,8(27),9,11,16,21,23-decaene (SB1317/TG02), a potent inhibitor of cyclin dependent kina 2. Pasha MK, et al. Preclinical metabolism and pharmacokinetics of SB1317 (TG02), a potent CDK/JAK2/FLT3 inhibitor. Drug Metab Lett. 2012 Mar;6(1):33-42.

Related compound libraries

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

(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 Cyclin dependent kinase FLT3 Janus kinase (E/Z)-SB1317 CD135 leukemias Inhibitor (E/Z)-TG02 CDK2 Cluster of differentiation antigen 135 inhibit cancer (E/Z) Zotiraciclib (E/Z)Zotiraciclib inhibitor

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