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SB1317

Cat No.
CEI-1520
Product Overview
SB1317 is a potent inhibitor of Cyclin dependent kinases (CDKs), FMS-like tyrosine kinase-3 (FLT3) and Janus kinase 2 (JAK2) with IC50 values of 13nM, 56nM and 73nM for CDK2, JAK2 and FLT3, respectively. CDKs are serine-threonine kinases that regulating the cell cycle. JAK2 is a nonreciprocal intracellular tyrosine kinase that transduces cytokine-mediated signals via the JAK-STAT pathway. FLT3 is a cytokine receptor and plays an important role in the normal development of haematopoietic stem cells. In luciferase-expressing MM1S cells, SB1317 overcame the proliferative/protective advantage conferred by IL-6.In MM1S cells, SB1317 increased the percentage of cells in G2/M phases and decreased cells in the S phase. Also, SB1317 increased the amount of cells in the subG0 region. In CB17-SCID mice bearing human multiple myeloma plasmacytoma xenograft models (the bortezomib-sensitive MM1S model and the more bortezomib-resistant OPM2 model), SB1317 significantly inhibited tumor growth. In a subcutaneous AML model, treatment mice with SB1317 dosed 10, 20 or 40 mg/kg daily for 21 days reduced the average tumor volume by 53%, 61% and 113%, respectively.
CAS No.
937270-47-8
Molecular Weight
372.46
Purity
0.98
Storage
Store at -20°C
Synonyms
TG02; SB 1317; TG 02; SB-1317; TG-02
Targets
CDK
Molecular Formula
C23H24N4O
Solubility
Soluble in DMSO
Shipping Conditions
Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request
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