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Products are for research use only. Not for human use. We do not sell to patients.
(TG02; SB 1317; TG 02; SB-1317; TG-02)
SB1317 Chemical Structure
|Product name: SB1317|
|Cat. No.: HY-15166|
|ABT-263||≤1 nM, Ki||≤1 nM, Ki|
SB1317(TG-02) is a novel small molecule potent CDK2/JAK2/FLT3 inhibitor with IC50s of 13/73/56 nM respectively.
IC50 Value: 13/73/56 nM(CDK2/JAK2/FLT3)
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 being CDKs. TG02 is anti-proliferative in a broad range of tumor cell lines, inducing G1 cell cycle arrest and apoptosis. In vivo, TG02 exhibits favorable pharmacokinetics after oral dosing in xenograft models and accumulates in tumor tissues, inducing an effective blockade of both CDK and STAT signaling. TG02 induces tumor regression after oral dosing on both daily and intermittent schedules in a murine model of mutant-FLT3 leukemia (MV4-11) and prolongs survival in a disseminated AML model with wild-type FLT3 and JAK2 (HL-60). TG02 is active in various models of leukemia and provide a rationale for the ongoing clinical evaluation of TG02 in patients with advanced leukemias.
|M.Wt||372.46||Storage||Please store the product under the recommended conditions in the Certificate of Analysis.|
|Solvent & Solubility||
DMSO: ≥ 49 mg/mL
|1 mg||5 mg||10 mg|
|1 mM||2.6849 mL||13.4243 mL||26.8485 mL|
|5 mM||0.5370 mL||2.6849 mL||5.3697 mL|
|10 mM||0.2685 mL||1.3424 mL||2.6849 mL|
|Product Name||Sponsor Only||Condition||Start Date||End Date||Phase||Last Change Date|
|SB1317||Tragara Pharmaceuticals Inc||Hematological neoplasm||31-AUG-10||31-JUL-13||Phase 1||14-NOV-13|
|Tragara Pharmaceuticals Inc||Chronic lymphocytic leukemia||30-SEP-12||31-AUG-14||Phase 1||14-NOV-13|
. William AD, Lee AC, Goh KC et al. Discovery of kinase spectrum selective macrocycle (16E)-14-methyl-20-oxa-5,7,14,26-tetraazatetracyclo[188.8.131.52(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. 2012 Jan 12;55(1):169-96.
. Poulsen A, William A, Blanchard S et al. 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. 2012 Jul 22.
AG-490 (Tyrphostin AG 490) is an inhibitor of EGFR with IC50 of 0.1 (mu)M, 135-fold more selective for EGFR versus ErbB2, also inhibits JAK2 with no activity to Lck, Lyn, Btk, Syk and Src.
AMG 925 is a potent and selective dual inhibtor of CDK4/FLT3 with IC50s of 1.5 nM and 2.4 nM for CDK4 and FLT3, respectively; with IC50 of 19 nM in MOLM-13 cell.
Amuvatinib (MP-470) is a potent and multi-targeted inhibitor of c-Kit, PDGFR(alpha) and Flt3 with IC50 of 10 nM, 40 nM and 81 nM, respectively.
AST487(NVP-AST487) is a Ret kinase inhibitor/FLT3 inhibitor with IC50 of 0.88 uM for Ret.
AT9283 is a small molecule a multi-targeted inhibitor with IC50s of 4, 1.2, 1.1 and approximate 3 nM for Bcr-Abl(T3151), JAK2 and JAK3, Aurora A and Aurora B, respectively.
AZD1480 is a novel ATP-competitive JAK2 inhibitor with IC50 of 0.26 nM, selectivity against JAK3 and Tyk2, and to a smaller extent against JAK1.
AZD5438 is a potent inhibitor of CDK1/2/9 with IC50 of 16 nM/6 nM/20 nM. It is less potent to CDK5/6.
6-BIO(6-Bromoindirubin-3(acute)-oxime) is a potent and selective inhibitor of GSK-3 and CDK1–cyclinB complex with IC50 of 5 nM /320 nM/83 nM for GSK-3(alpha)(beta)/CDK1/CDK5 respectively.
BMS-265246 is a potent and selective CDK1/2 inhibitor for CDK1/cyclin B and CDK2/cyclin E with IC50 of 6 nM and 9 nM, respectively.
BMS-911543 is a potent and selective small-molecule inhibitor of JAK2, displays potent anti-proliferative and pharmacodynamic (PD) effects in cell lines dependent upon JAK2 signaling.
|Compound Name||Bcl-2||Bcl-B||Bcl-w||Bcl-xL||Mcl-1||Bfl-1||Other target||Note|
|ABT-737||30.3 nM||78.7 nM||197.8 nM|
|ABT-263||≤1 nM, Ki||≤1 nM, Ki||≤0.5 nM, Ki|
|Obatoclax||3 uM||2.9 uM||5 uM|
|TW-37||290 nM Ki||1110 nM, Ki||360 nM, Ki|
|ABT-199||10 nM, Ki||>10 uM, Ki||>10 uM, Ki||No inhibition||Bcl-2 selective|
|AT101||320 nM, Ki||480 nM, Ki||180 nM, Ki|
|Gambogic Acid||1.21 uM||0.66 uM||2.02 uM||1.47 uM||0.79 uM||1.06 uM||Caspase|
|(+)-Apogossypol||0.5-2 uM||0.5-2 uM||0.5-2 uM||0.5-2 uM||0.5-2 uM||No inhibition|
|Mcl1-IN-1||No inhibition||2.4 uM||Mcl1 selective|
|MIM1||>50 uM||4.8 uM||Mcl1 selective|
|Pyridoclax||25 nM, Kd|