Determine the necessary mass, volume, or concentration for preparing a solution.
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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S127924-5mg | 5mg | In stock | $107.90 | |
S127924-10mg | 10mg | In stock | $147.90 | |
S127924-25mg | 25mg | In stock | $333.90 | |
S127924-50mg | 50mg | In stock | $444.90 | |
S127924-100mg | 100mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $642.90 |
Synonyms | NSC762673 | NSC-762673 | EX-A7310 | 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- | TG02 | 1204918-72-8 | AC-35951 | BS167349 | (E)-6-methyl-12-oxa-3,6-diaza-2(4,2)-pyrimidina-1,4( |
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Specifications & Purity | Moligand™, ≥98% |
Biochemical and Physiological Mechanisms | TG02 is a novel pyrimidine-based multi-kinase inhibitor that inhibits CDKs 1, 2, 7 and 9 together with JAK2 and FLT3. It dose-dependently inhibits signaling pathways downstream of CDKs, JAK2 and FLT3 in cancer cells with the main targets |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Action Type | INHIBITOR |
Mechanism of action | Tyrosine-protein kinase JAK2 inhibitor |
ALogP | 4.2 |
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Mechanism of Action | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | References |
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IUPAC Name | (16E)-14-methyl-20-oxa-5,7,14,27-tetrazatetracyclo[19.3.1.12,6.18,12]heptacosa-1(25),2(27),3,5,8,10,12(26),16,21,23-decaene |
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INCHI | InChI=1S/C23H24N4O/c1-27-13-3-2-4-14-28-21-10-6-8-19(16-21)22-11-12-24-23(26-22)25-20-9-5-7-18(15-20)17-27/h2-3,5-12,15-16H,4,13-14,17H2,1H3,(H,24,25,26)/b3-2+ |
InChi Key | VXBAJLGYBMTJCY-NSCUHMNNSA-N |
Canonical SMILES | CN1CC=CCCOC2=CC=CC(=C2)C3=NC(=NC=C3)NC4=CC=CC(=C4)C1 |
Isomeric SMILES | CN1C/C=C/CCOC2=CC=CC(=C2)C3=NC(=NC=C3)NC4=CC=CC(=C4)C1 |
PubChem CID | 16739650 |
Molecular Weight | 372.46 |
PubChem CID | 16739650 |
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ChEMBL Ligand | CHEMBL1944698 |
BindingDB Ligand | 50363196 |
CAS Registry No. | 937270-47-8 |
Enter Lot Number to search for COA:
Find and download the COA for your product by matching the lot number on the packaging.
Lot Number | Certificate Type | Date | Item |
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C2212050 | Certificate of Analysis | Dec 20, 2023 | S127924 |
C2212111 | Certificate of Analysis | Dec 20, 2023 | S127924 |
C2212112 | Certificate of Analysis | Dec 20, 2023 | S127924 |
C2212135 | Certificate of Analysis | Dec 20, 2023 | S127924 |
C2214272 | Certificate of Analysis | Dec 20, 2023 | S127924 |
Solubility | insoluble in H2O; ≥44.87 mg/mL in DMSO; ≥3.98 mg/mL in EtOH with gentle warming and ultrasonic |
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1. William AD, Lee AC, Goh KC, Blanchard S, Poulsen A, Teo EL, Nagaraj H, Lee CP, Wang H, Williams M et al.. (2012) 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 kinases (CDKs), Janus kinase 2 (JAK2), and fms-like tyrosine kinase-3 (FLT3) for the treatment of cancer.. J Med Chem, 55 (1): (169-96). [PMID:22148278] [10.1021/op500134e] |
2. Goh KC, Novotny-Diermayr V, Hart S, Ong LC, Loh YK, Cheong A, Tan YC, Hu C, Jayaraman R, William AD et al.. (2012) TG02, a novel oral multi-kinase inhibitor of CDKs, JAK2 and FLT3 with potent anti-leukemic properties.. Leukemia, 26 (2): (236-43). [PMID:21860433] [10.1021/op500134e] |
3. Poulsen A, William A, Blanchard S, Nagaraj H, Williams M, Wang H, Lee A, Sun E, Teo EL, Tan E et al.. (2013) 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, 19 (1): (119-30). [PMID:22820730] [10.1021/op500134e] |
4. Pallis M, Abdul-Aziz A, Burrows F, Seedhouse C, Grundy M, Russell N. (2012) 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, 159 (2): (191-203). [PMID:22934750] [10.1021/op500134e] |
5. Pallis M, Burrows F, Whittall A, Boddy N, Seedhouse C, Russell N. (2013) Efficacy of RNA polymerase II inhibitors in targeting dormant leukaemia cells.. BMC Pharmacol Toxicol, 14 (13): (32). [PMID:23767415] [10.1021/op500134e] |