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    Zotiraciclib (TG-02, SB-1317)
    Zotiraciclib (TG-02, SB-1317)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V7667
    CAS #: 1204918-72-8Purity ≥98%

    Description: Zotiraciclib (formerly TG02, SB1317) is an orally bioavailable, brain penetrant and multi-kinase (CDK/JAK2/FLT3) inhibitor for the treatment of cancer (e.g.  anaplastic astrocytoma and GBM, as well as DIPG, a rare pediatric cance). It is a small molecule macrocyclic compound that was discovered by S*BIO Pte Ltd in Singapore. It crosses the BBB (blood brain barrier) and acts by depleting Myc through the inhibition of cyclin-dependent kinase 9 (CDK9). It is one of the many CDK inhibitors under investigation for cancer treatment; others targeting CDK9 for the treatment of acute myeloid leukemia (AML) include alvocidib and atuveciclib. Myc overexpression is a known factor in various cancers, with 80 percent of glioblastomas characterized by this property. Zotiraciclib has been granted orphan drug designation by the US Food and Drug Administration (FDA) and the European Medicines Agency (EMA) for the treatment of gliomas.

    References: 

    1. The multi-kinase inhibitor TG02 overcomes signalling activation by survival factors to deplete MCL1 and XIAP and induce cell death in primary acute myeloid leukaemia cells. Br J Haematol. 2012 Oct;159(2):191-203. 

    2. Structure-based design of nitrogen-linked macrocyclic kinase inhibitors leading to the clinical candidate SB1317/TG02, a potent inhibitor of cyclin dependant kinases (CDKs), Janus kinase 2 (JAK2), and Fms-like tyrosine kinase-3 (FLT3). J Mol Model. 2013 Jan;19(1):119-30. 

    3. Preclinical metabolism and pharmacokinetics of SB1317 (TG02), a potent CDK/JAK2/FLT3 inhibitor. Drug Metab Lett. 2012 Mar;6(1):33-42. 

    4. 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)]heptaco sa-1(25),2(26),3,5,8(27),9,11,16,21,23-decaene (SB1317/TG02), a potent inhibitor of cyclin dependent kinases (CDKs), Janus kinase 2 (JAK2), and fms-like tyrosine kinase-3 (FLT3) for the treatment of cancer. J Med Chem. 2012 Jan 12;55(1):169-96. 

    Related CAS #: 1204918-72-8 (free base)   1354567-82-0 (HCl)   1204918-73-9 (citrate)    937270-47-8 (free base)    

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    Molecular Formula: C23H24N4O
    Exact Mass: 372.19501
    Molecular Weight: 372.46 

    Synonym: TG02;  Ex45;SB1317; SB1317; SB 1317;  Ex-45; EX 45; TG 02; TG02; 


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