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CRT0066101

Name: CRT0066101
Brand: TargetMol
SKU: T86093
Rating: 4.5 (1 reviews)

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Catalog No. T86093Cas No. 956123-34-5

Alias 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

😃Good

Catalog No. T86093Alias CRT-0066101, CRT 0066101Cas No. 956123-34-5

Pack Size	Price	USA Warehouse	Global Warehouse	Quantity
10 mg	Inquiry	10-14 weeks	10-14 weeks
50 mg	Inquiry	10-14 weeks	10-14 weeks

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

Questions

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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	PKD1:1 nM, PKD2:2.5 nM, PKD3:2 nM
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].
Synonyms	CRT-0066101, CRT 0066101

Chemical Properties

Molecular Weight	338.41
Formula	C₁₈H₂₂N₆O
Cas No.	956123-34-5
Smiles	OC=1C(=CC(=CC1)C2=CN(C)N=C2)C=3N=C(NC[C@@H](CC)N)C=CN3

Storage & Solubility Information

Storage

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

	1mg	5mg	10mg	50mg
1 mM	2.9550 mL	14.7750 mL	29.5500 mL	147.7498 mL
5 mM	0.5910 mL	2.9550 mL	5.9100 mL	29.5500 mL
10 mM	0.2955 mL	1.4775 mL	2.9550 mL	14.7750 mL
20 mM	0.1477 mL	0.7387 mL	1.4775 mL	7.3875 mL
50 mM	0.0591 mL	0.2955 mL	0.5910 mL	2.9550 mL
100 mM	0.0295 mL	0.1477 mL	0.2955 mL	1.4775 mL

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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:

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 DMSO TargetMol | 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 DMSO TargetMol | reagent stock solution to 400 μL PEG300 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 ddH₂O TargetMol | 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.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

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

CRT0066101

CRT0066101

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In Vivo Formulation Calculator (Clear solution)

Dose Conversion

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