SB1317

• CAT Number: I000032
• CAS Number: 937270-47-8
• Molecular Formula: C23H24N4O
• Molecular Weight: 372.47
• Purity: ≥95%
• Synonyms: TG02; TG 02; TG02; SB1317; SB1317; SB 1317.
• Target: JAK
• Solubility: DMSO: ≤ 26.5 mg/mL
• Storage: Store at -20°C
• IC50: 13/73/56 nM(CDK2/JAK2/FLT3)
• 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
• 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+
• InChIKey: VXBAJLGYBMTJCY-NSCUHMNNSA-N
• SMILES: CN1CC=CCCOC2=CC=CC(=C2)C3=NC(=NC=C3)NC4=CC=CC(=C4)C1

SB1317（Cat No.:I000032）, also known as Dihydrochloride, is a potent and selective inhibitor of cyclin-dependent kinase 9 (CDK9), a key regulator of transcriptional elongation. It inhibits CDK9 with an IC50 of 13 nM, leading to the suppression of RNA polymerase II-dependent transcription and the downregulation of various oncogenes. SB1317 has shown anticancer activity in preclinical studies, making it a promising candidate for the treatment of various malignancies, including hematological cancers and solid tumors.

Reference

1: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). Poulsen A, William A, Blanchard S, Nagaraj H, Williams M, Wang H, Lee A, Sun E, Teo EL, Tan E, Goh KC, Dymock B.J Mol Model. 2013 Jan;19(1):119-30. doi: 10.1007/s00894-012-1528-7. Epub 2012 Jul 22. PMID: 22820730
2:Preclinical metabolism and pharmacokinetics of SB1317 (TG02), a potent CDK/JAK2/FLT3 inhibitor. Pasha MK, Jayaraman R, Reddy VP, Yeo P, Goh E, Williams A, Goh KC, Kantharaj E.Drug Metab Lett. 2012 Mar;6(1):33-42. PMID: 22372550
3: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. William AD, Lee AC, Goh KC, Blanchard S, Poulsen A, Teo EL, Nagaraj H, Lee CP, Wang H, Williams M, Sun ET, Hu C, Jayaraman R, Pasha MK, Ethirajulu K, Wood JM, Dymock BW.J Med Chem. 2012 Jan 12;55(1):169-96. doi: 10.1021/jm201112g. Epub 2011 Dec 29. PMID: 22148278