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

CRT0066101 is a potent and orally active PKD inhibitor with IC50 values of 1 nM, 2.5 nM and 2 nM for PKD1, PKD2, and PKD3, respectively. CRT0066101 is also a potent PIM2 inhibitor with an IC50 of ~135.7 nM. CRT0066101 has anticancer effects.

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CRT0066101 Chemical Structure

CRT0066101 Chemical Structure

CAS No. : 956123-34-5

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Based on 2 publication(s) in Google Scholar

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Description

CRT0066101 is a potent and orally active PKD inhibitor with IC50 values of 1 nM, 2.5 nM and 2 nM for PKD1, PKD2, and PKD3, respectively[1]. CRT0066101 is also a potent PIM2 inhibitor with an IC50 of ~135.7 nM. CRT0066101 has anticancer effects[2].

IC50 & Target[1][2]

PKD1

1 nM (IC50)

PKD2

2.5 nM (IC50)

PKD3

2 nM (IC50)

PIM2

135.7 nM (IC50)

In Vitro

CRT0066101 (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 significantly inhibits Panc-1 cell proliferation, with an IC50 value of 1 µM. CRT0066101 results in a 6-10 fold induction of apoptosis in Panc-1 cells. CRT0066101 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 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 (80 mg/kg/day; oral gavage; once daily; for 21 days) in Panc-1 orthotopic model potently blocks tumor growth in vivo[1].

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.
Molecular Weight

338.41

Formula

C18H22N6O
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

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
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (295.50 mM; Need ultrasonic; 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 2.9550 mL 14.7750 mL 29.5500 mL
5 mM 0.5910 mL 2.9550 mL 5.9100 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. 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: ≥ 2.5 mg/mL (7.39 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (7.39 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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).
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. 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 2.9550 mL 14.7750 mL 29.5500 mL 73.8749 mL
5 mM 0.5910 mL 2.9550 mL 5.9100 mL 14.7750 mL
10 mM 0.2955 mL 1.4775 mL 2.9550 mL 7.3875 mL
15 mM 0.1970 mL 0.9850 mL 1.9700 mL 4.9250 mL
20 mM 0.1477 mL 0.7387 mL 1.4775 mL 3.6937 mL
25 mM 0.1182 mL 0.5910 mL 1.1820 mL 2.9550 mL
30 mM 0.0985 mL 0.4925 mL 0.9850 mL 2.4625 mL
40 mM 0.0739 mL 0.3694 mL 0.7387 mL 1.8469 mL
50 mM 0.0591 mL 0.2955 mL 0.5910 mL 1.4775 mL
60 mM 0.0492 mL 0.2462 mL 0.4925 mL 1.2312 mL
80 mM 0.0369 mL 0.1847 mL 0.3694 mL 0.9234 mL
100 mM 0.0295 mL 0.1477 mL 0.2955 mL 0.7387 mL
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CRT0066101 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:

CRT0066101956123-34-5CRT 0066101CRT-0066101PKDPimApoptosisProtein kinase DPim kinasesPKD1PKD2PKD3PIM2anticancer effectspS82-Hsp27Inhibitorinhibitorinhibit

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