SB1317 - CAS 1204918-72-8
Catalog number: B0084-457585
Category: Inhibitor
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SB1317 is a novel small molecule potent CDK/JAK2/FLT3 inhibitor. It dose-dependently inhibits signaling pathways downstream of CDKs, JAK2 and FLT3 in cancer cells with the main targets being CDKs. SB1317 is anti-proliferative in a broad range of tumor cell lines, inducing G1 cell cycle arrest and apoptosis. In vivo, SB1317 exhibits favorable pharmacokinetics after oral dosing in xenograft models and accumulates in tumor tissues, inducing an effective blockade of both CDK and STAT signaling. SB1317 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). SB1317 is active in various models of leukemia and provide a rationale for the ongoing clinical evaluation of TG02 in patients with advanced leukemias.
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B0084-457585 20 mg $199 In stock
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Brife Description:
CDK/JAK2/FLT3 inhibitor
Related CAS:
white solid powder
TG02; TG 02; TG-02; SB1317 (Double bond E); TG02 (Double bond E)
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Current Developer:
Tragara Pharmaceuticals, Inc.
1.Efficacy of RNA polymerase II inhibitors in targeting dormant leukaemia cells.
Pallis M, Burrows F, Whittall A, Boddy N, Seedhouse C, Russell N. BMC Pharmacol Toxicol. 2013 Jun 15;14:32. doi: 10.1186/2050-6511-14-32.
BACKGROUND: Dormant cells are characterised by low RNA synthesis. In contrast, cancer cells can be addicted to high RNA synthesis, including synthesis of survival molecules. We hypothesised that dormant cancer cells, already low in RNA, might be sensitive to apoptosis induced by RNA Polymerase II (RP2) inhibitors that further reduce RNA synthesis.
2.Discovery of kinase spectrum selective macrocycle (16E)-14-methyl-20-oxa-5,7,14,26-tetraazatetracyclo[,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 AD1, 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.
Herein, we describe the design, synthesis, and SAR of a series of unique small molecule macrocycles that show spectrum selective kinase inhibition of CDKs, JAK2, and FLT3. The most promising leads were assessed in vitro for their inhibition of cancer cell proliferation, solubility, CYP450 inhibition, and microsomal stability. This screening cascade revealed 26 h as a preferred compound with target IC(50) of 13, 73, and 56 nM for CDK2, JAK2 and FLT3, respectively. Pharmacokinetic (PK) studies of 26 h in preclinical species showed good oral exposures. Oral efficacy was observed in colon (HCT-116) and lymphoma (Ramos) xenograft studies, in line with the observed PK/PD correlation. 26h (SB1317/TG02) was progressed into development in 2010 and is currently undergoing phase 1 clinical trials in advanced leukemias and multiple myeloma.
3.Potent antimyeloma activity of a novel ERK5/CDK inhibitor.
Álvarez-Fernández S1, Ortiz-Ruiz MJ, Parrott T, Zaknoen S, Ocio EM, San Miguel J, Burrows FJ, Esparís-Ogando A, Pandiella A. Clin Cancer Res. 2013 May 15;19(10):2677-87. doi: 10.1158/1078-0432.CCR-12-2118. Epub 2013 Mar 26.
PURPOSE: To analyze the antimyeloma potential of TG02, an ERK5/CDK inhibitory drug.
4.Acid Mediated Ring Closing Metathesis: A Powerful Synthetic Tool Enabling the Synthesis of Clinical Stage Kinase Inhibitors.
William AD1, Lee AC2. Chimia (Aarau). 2015;69(3):142-5. doi: 10.2533/chimia.2015.142.
The powerful olefin metathesis reaction was employed for the construction of late-phase clinical agents SB1317 and SB1518. In both cases RCM seems to proceed only in the presence of an acid and to predominantly furnish trans isomers. In case of SB1518 it proceeded in the presence of acid HCl, while for SB1317, it mainly proceeds in the presence of TFA (trifluroacetic acid).
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CAS 1204918-72-8 SB1317

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