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KT-333

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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

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Purity: 98.12%
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 SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$413In StockIn Stock
5 mg$828In StockIn Stock
10 mg$1,160In StockIn Stock
25 mg$1,880-In Stock
50 mg$2,670InquiryInquiry
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:98.12%
Appearance:Solid
Color:White
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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].
SynonymsKT333
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 | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 100 mg/mL (79.51 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM0.7951 mL3.9753 mL7.9505 mL39.7526 mL
5 mM0.1590 mL0.7951 mL1.5901 mL7.9505 mL
10 mM0.0795 mL0.3975 mL0.7951 mL3.9753 mL
20 mM0.0398 mL0.1988 mL0.3975 mL1.9876 mL
50 mM0.0159 mL0.0795 mL0.1590 mL0.7951 mL

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Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
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