2. Apoptosis JAK/STAT Signaling
  3. PKD Pim Apoptosis
  4. CRT0066101 trihydrochloride

CRT0066101 trihydrochloride is the trihydrochloride salt form of CRT0066101 (HY-15698). CRT0066101 trihydrochloride is an orally active PKD inhibitor with IC50 values of 1 nM, 2.5 nM and 2 nM for PKD1, PKD2, and PKD3, respectively. CRT0066101 trihydrochloride is also an inhibitor for PIM2 with an IC50 of ~135.7 nM. CRT0066101 trihydrochloride exhibits anti-inflammatory activity in mice LPS (HY-D1056)-induced lung injury models, and has anticancer effects.

For research use only. We do not sell to patients.

CRT0066101 trihydrochloride

CRT0066101 trihydrochloride Chemical Structure

CAS No. : 1781742-22-0

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Other In-stock Forms of CRT0066101 trihydrochloride:

Other Forms of CRT0066101 trihydrochloride:

CRT0066101 trihydrochloride Related Antibodies

Top Publications Citing Use of Products

View All PKD Isoform Specific Products:

View All Isoforms
PKD1 PKD2 PKD3

View All Pim Isoform Specific Products:

View All Isoforms
PIM1 PIM2 PIM3

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

CRT0066101 trihydrochloride is the trihydrochloride salt form of CRT0066101 (HY-15698). CRT0066101 trihydrochloride is an orally active PKD inhibitor with IC50 values of 1 nM, 2.5 nM and 2 nM for PKD1, PKD2, and PKD3, respectively. CRT0066101 trihydrochloride is also an inhibitor for PIM2 with an IC50 of ~135.7 nM. CRT0066101 trihydrochloride exhibits anti-inflammatory activity in mice LPS (HY-D1056)-induced lung injury models, and has anticancer effects[1][2][3].

IC50 & Target

PKD1/PKCμ

1 nM (IC50)

PKD3

2 nM (IC50)

PKD2

2.5 nM (IC50)

PIM2

135.7 nM (IC50)

In Vitro

CRT0066101 trihydrochloride (5 µM; 1 h) blockS both the basal and NT-induced pS916-PKD1/2 (activated PKD1/2) in Panc-1 and Panc-28 cells. CRT0066101 abrogates NT-induced phosphorylation of Hsp27 (pS82-Hsp27), attenuates PKD1-mediated NF-κB activation, and abrogates expression of NF-κB-dependent-dependent proliferative and pro-survival proteins[1].
CRT0066101 trihydrochloride significantly inhibits Panc-1 cell proliferation, with an IC50 value of 1 µM. CRT0066101 trihydrochloride results in a 6-10 fold induction of apoptosis in Panc-1 cells. CRT0066101 trihydrochloride significantly reduces cell proliferation of Colo357, Panc-1, MiaPaCa-2, and AsPC-1 cells but had a modest effect in Capan-2 cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

CRT0066101 trihydrochloride Related Antibodies

Western Blot Analysis[1]

Cell Line: Panc-1 and Panc-28 cells stimulation with neurotensin (NT)
Concentration: 5 µM
Incubation Time: 1 h
Result: Blocked both the basal and NT-induced pS916-PKD1/2 (activated PKD1/2).
In Vivo

CRT0066101 trihydrochloride (80 mg/kg/day; oral gavage; once daily; for 21 days) in Panc-1 orthotopic model potently blocks tumor growth in vivo[1].
CRT0066101 trihydrochloride (10 mg/kg, i.p., every two days for 3 times) exhibits a protective effect against LPS-induced pneumonia and alleviates lung damage in C57BL/6J mice[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: CR-UK nu/nu mice injected with Panc-1 cells[1]
Dosage: 80 mg/kg/day
Administration: Oral gavage; once daily; for 21 days
Result: Potently blocked tumor growth in vivo.
Animal Model: LPS (HY-D1056)-induced lung injury in C57BL/6J mice[3]
Dosage: 10 mg/kg
Administration: i.p., once every two days for 3 times
Result: Inhibited the expression of MyD88 and TLR4, inhibited the phosphorylation of NF-κB, ERK and JNK.
Molecular Weight

447.79

Formula

C18H25Cl3N6O
CAS No.
Appearance

Solid

SMILES

[H]Cl.[H]Cl.[H]Cl.N[C@H](CC)CNC1=NC(C2=C(O)C=CC(C3=CN(C)N=C3)=C2)=NC=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 20 mg/mL (44.66 mM; warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2332 mL 11.1659 mL 22.3319 mL
5 mM 0.4466 mL 2.2332 mL 4.4664 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2 mg/mL (4.47 mM); Clear solution

    This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2 mg/mL (4.47 mM); Clear solution

    This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2332 mL 11.1659 mL 22.3319 mL 55.8297 mL
5 mM 0.4466 mL 2.2332 mL 4.4664 mL 11.1659 mL
10 mM 0.2233 mL 1.1166 mL 2.2332 mL 5.5830 mL
15 mM 0.1489 mL 0.7444 mL 1.4888 mL 3.7220 mL
20 mM 0.1117 mL 0.5583 mL 1.1166 mL 2.7915 mL
25 mM 0.0893 mL 0.4466 mL 0.8933 mL 2.2332 mL
30 mM 0.0744 mL 0.3722 mL 0.7444 mL 1.8610 mL
40 mM 0.0558 mL 0.2791 mL 0.5583 mL 1.3957 mL
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

CRT0066101 trihydrochloride Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

CRT0066101 trihydrochloride1781742-22-0PKDPimApoptosisProtein kinase DPim kinasesPKD1PKD2PKD3PIM2anticancer effectspS82-Hsp27C57BL/6J mouseanti-inflammatoryInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
CRT0066101 trihydrochloride
Cat. No.:
HY-15698B
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.