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KT-333 is a potent, highly selective, heterobifunctional small molecule degrader of STAT3 for the treatment of a variety of STAT3-dependent pathologies, including hematologic malignancies and solid tumors.KT-333 specifically binds to STAT3 proteins at one end of the spectrum, and binds to the E3 ubiquitin ligase, VHL, at the other end.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $413 | In Stock | |
5 mg | $987 | In Stock | |
10 mg | $1,680 | In Stock | |
25 mg | $2,520 | In Stock | |
50 mg | $3,380 | In Stock |
Description | KT-333 is a potent, highly selective, heterobifunctional small molecule degrader of STAT3 for the treatment of a variety of STAT3-dependent pathologies, including hematologic malignancies and solid tumors.KT-333 specifically binds to STAT3 proteins at one end of the spectrum, and binds to the E3 ubiquitin ligase, VHL, at the other end. |
In vitro | KT-333 is a PROTAC targeting STAT3 with a VHL-dependent mechanism that is in Phase 1a/1b trials for the treatment of multiple diseases, including R/R B-cell and T-cell lymphomas, classical Hodgkin lymphoma (cHL), solid tumors (ST), and large granular lymphocytic leukemia/T-cell prolymphocytic leukemia (LGL-L/T-PLL).[1] |
In vivo | KT-333 ammonium, administered intravenously at doses of 5, 10, 15, and 45 mg/kg once a week for two weeks, exhibited dose-dependent antitumor activity. Mice receiving 5 mg/kg achieved 79.9% tumor growth inhibition (TGI), while complete tumor regression was observed in those given 10, 15, or 45 mg/kg, with effects lasting until the end of the study [1]. Similarly, KT-333 ammonium at 10, 20, and 30 mg/kg showed dose-dependent antitumor effects over the same administration schedule. Mice treated with 10 mg/kg exhibited 83.8% TGI, and complete tumor regression was seen at 20 or 30 mg/kg, with sustained effects [1]. |
Alias | KT333 |
Molecular Weight | 1257.78 |
Formula | C60H74ClN10O14PS |
Cas No. | 2502186-79-8 |
Smiles | C(N[C@H](COC1=C(Cl)C(CCCC(N[C@H](C(=O)N2[C@H](C(N[C@@H](C)C3=CC=C(C=C3)C4=C(C)N=CS4)=O)C[C@@H](O)C2)C(C)(C)C)=O)=CC=C1)CCC(N)=O)(=O)[C@H]5N6[C@](CC5)(CCN(C(C)=O)C[C@H](NC(=O)C7=CC=8C(N7)=CC=C(C(P(=O)(O)O)=O)C8)C6=O)[H] |
Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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