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Zotiraciclib

Chemical Structure : Zotiraciclib

CAS No.: 937270-47-8

Zotiraciclib (TG02, (E/Z)-TG02, (E/Z)-SB1317)

Catalog No.: PC-38758Not For Human Use, Lab Use Only.

Zotiraciclib (TG02, SB1317) is a potent multi-kinase inhibitor of cyclin dependent kinases (CDKs), JAK2, and FLT3 with IC50of 13, 73, and 56 nM for CDK2, JAK2 and FLT3, respectively.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Zotiraciclib (TG02, SB1317) is a potent multi-kinase inhibitor of cyclin dependent kinases (CDKs), JAK2, and FLT3 with IC50of 13, 73, and 56 nM for CDK2, JAK2 and FLT3, respectively.
Zotiraciclib (TG02, SB1317) is anti-proliferative in a broad range of tumor cell lines, inducing G1 cell cycle arrest and apoptosis.
Zotiraciclib (TG02, SB1317) shows high sensitivity to primary cultures of progenitor cells derived from acute myeloid leukemia (AML) and polycythemia vera patients.
Zotiraciclib (TG02, SB1317) exhibits favorable pharmacokinetics after oral dosing in xenograft models and accumulates in tumor tissues, inducing an effective blockade of both CDK and STAT signaling.
Zotiraciclib (TG02, SB1317) also shows oral efficacy in colon (HCT-116) and lymphoma (Ramos) xenografts.

Physicochemical Properties

M.Wt 372.46
Formula C23H24N4O
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

20-Oxa-5,7,14,27-tetraazatetracyclo[19.3.1.12,6.18,12]heptacosa-1(25),2,4,6(27),8,10,12(26),16,21,23-decaene, 14-methyl-

References

1. Ortiz-Ruiz MJ, et al. Oncotarget. 2014 Nov 30;5(22):11308-18.

2. Poulsen A, et al. J Mol Model. 2013 Jan;19(1):119-30.

3. William AD, et al. J Med Chem. 2012 Jan 12;55(1):169-96.

4. Goh KC, et al. Leukemia. 2012 Feb;26(2):236-43.

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