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CRT0066101 (Synonyms: CRT-0066101, CRT 0066101)

Catalog No. T86093 Copy Product Info
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CRT0066101 is a potent and orally active protein kinase D inhibitor with low-nanomolar activity against PKD1, PKD2, and PKD3, while also inhibiting PIM2, CRT0066101 demonstrates significant anti-inflammatory efficacy in lipopolysaccharide-induced lung injury models as well as anticancer activity, supporting its use in inflammation and oncology research.

CRT0066101

Copy Product Info
🥰Excellent
Catalog No. T86093
Synonyms CRT-0066101, CRT 0066101

CRT0066101 is a potent and orally active protein kinase D inhibitor with low-nanomolar activity against PKD1, PKD2, and PKD3, while also inhibiting PIM2, CRT0066101 demonstrates significant anti-inflammatory efficacy in lipopolysaccharide-induced lung injury models as well as anticancer activity, supporting its use in inflammation and oncology research.

CRT0066101
Cas No. 956123-34-5
Pack SizePriceUSA StockGlobal StockQuantity
10 mgInquiry10-14 weeks10-14 weeks
50 mgInquiry10-14 weeks10-14 weeks
For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)
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For research use only—not for human use. No sales to individuals. Use as intended only.
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Product Introduction

Bioactivity
Description
CRT0066101 is a potent and orally active protein kinase D inhibitor with low-nanomolar activity against PKD1, PKD2, and PKD3, while also inhibiting PIM2, CRT0066101 demonstrates significant anti-inflammatory efficacy in lipopolysaccharide-induced lung injury models as well as anticancer activity, supporting its use in inflammation and oncology research.
Targets&IC50
PKD3:2 nM, PKD2:2.5 nM, PKD1:1 nM, Panc-1 cells:1 μM, Panc-28 cells:1 μM
In vitro
In enzymatic assays, CRT0066101 inhibited the PKD family with IC50 values of 1 nM (PKD1), 2.5 nM (PKD2), and 2 nM (PKD3), as well as PIM2 (IC50 = 135.7 nM). In pancreatic cancer cell lines (Panc-1, Panc-28), CRT0066101 inhibited proliferation (IC50 ~ 1 μM), and induced a 6- to 10-fold increase in apoptosis [1].
In vivo
In a Panc-1 orthotopic xenograft model, oral administration of CRT0066101 (80 mg/kg/day) for 21 days blocked tumor growth. Additionally, in a mouse model of LPS-induced lung injury, intraperitoneal injection of CRT0066101 (10 mg/kg, every 2 days) reduced lung tissue damage and inhibited the cytokine storm [1][3].
SynonymsCRT-0066101, CRT 0066101
Chemical Properties
Molecular Weight338.41
FormulaC18H22N6O
Cas No.956123-34-5
SmilesOC=1C(=CC(=CC1)C2=CN(C)N=C2)C=3N=C(NC[C@@H](CC)N)C=CN3
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 80 mg/mL (236.4 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.9550 mL14.7750 mL29.5500 mL147.7498 mL
5 mM0.5910 mL2.9550 mL5.9100 mL29.5500 mL
10 mM0.2955 mL1.4775 mL2.9550 mL14.7750 mL
20 mM0.1477 mL0.7387 mL1.4775 mL7.3875 mL
50 mM0.0591 mL0.2955 mL0.5910 mL2.9550 mL
100 mM0.0295 mL0.1477 mL0.2955 mL1.4775 mL
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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In Vivo Formulation Calculator (Clear solution)

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:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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