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KT-333

🥰Excellent
Catalog No. T88358Cas No. 2502186-79-8
Alias KT333

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.

KT-333

KT-333

🥰Excellent
Catalog No. T88358Alias KT333Cas No. 2502186-79-8
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 SizePriceAvailabilityQuantity
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
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Product Introduction

Bioactivity
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].
AliasKT333
Chemical Properties
Molecular Weight1257.78
FormulaC60H74ClN10O14PS
Cas No.2502186-79-8
SmilesC(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 & Solubility Information
Storagestore at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

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