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SB1317 (TG02) is a novel pyrimidine-based multi-kinase inhibitor that inhibits CDKs 1, 2, 7 and 9 together with JAK2 and FLT3. SB1317 dose-dependently inhibits signaling pathways downstream of CDKs, JAK2 and FLT3 in cancer cells with the main targets being CDKs. 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). In vivo, SB1317 (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. SB1317 is currently undergoing phase 1 clinical trials in advanced leukemias and multiple myeloma.
| Molecular Weight | 372.46 |
| Formula | C23H24N4O |
| CAS Number | 937270-47-8 |
| Solubility (25°C) | DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[1] Yu-Ting Su, et al. Novel Targeting of Transcription and Metabolism in Glioblastoma
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