1. Apoptosis JAK/STAT Signaling
  2. PKD Pim Apoptosis
  3. CRT0066101 dihydrochloride

CRT0066101 dihydrochloride 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 dihydrochloride is also a potent PIM2 inhibitor with an IC50 of ~135.7 nM. CRT0066101 dihydrochloride has anticancer effects.

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

CRT0066101 dihydrochloride Chemical Structure

CRT0066101 dihydrochloride Chemical Structure

CAS No. : 1883545-60-5

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10 mM * 1 mL in DMSO
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Based on 2 publication(s) in Google Scholar

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Description

CRT0066101 dihydrochloride 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 dihydrochloride is also a potent PIM2 inhibitor with an IC50 of ~135.7 nM. CRT0066101 dihydrochloride has anticancer effects[2].

IC50 & Target[1][2]

PKD1

1 nM (IC50)

PKD3

2 nM (IC50)

PKD2

2.5 nM (IC50)

PIM2

135.7 nM (IC50)

In Vitro

CRT0066101 (5 µM; 1 h) dihydrochloride blockS both the basal and NT-induced pS916-PKD1/2 (activated PKD1/2) in Panc-1 and Panc-28 cells. CRT0066101 dihydrochloride 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 dihydrochloride significantly inhibits Panc-1 cell proliferation, with an IC50 value of 1 µM. CRT0066101 dihydrochloride results in a 6-10 fold induction of apoptosis in Panc-1 cells. CRT0066101 dihydrochloride 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.

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) dihydrochloride 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

411.33

Formula

C18H24Cl2N6O

CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

OC1=CC=C(C2=CN(C)N=C2)C=C1C3=NC=CC(NC[C@H](N)CC)=N3.[H]Cl.[H]Cl

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: 

H2O : 50 mg/mL (121.56 mM; Need ultrasonic)

DMSO : 11.36 mg/mL (27.62 mM; ultrasonic and 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 2.4311 mL 12.1557 mL 24.3114 mL
5 mM 0.4862 mL 2.4311 mL 4.8623 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.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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: ≥ 1.14 mg/mL (2.77 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.14 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (11.4 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: ≥ 1.14 mg/mL (2.77 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.14 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (11.4 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.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  PBS

    Solubility: 25 mg/mL (60.78 mM); Clear solution; Need ultrasonic

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.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
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).
Purity & Documentation

Purity: 99.92%

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 / H2O 1 mM 2.4311 mL 12.1557 mL 24.3114 mL 60.7785 mL
5 mM 0.4862 mL 2.4311 mL 4.8623 mL 12.1557 mL
10 mM 0.2431 mL 1.2156 mL 2.4311 mL 6.0778 mL
15 mM 0.1621 mL 0.8104 mL 1.6208 mL 4.0519 mL
20 mM 0.1216 mL 0.6078 mL 1.2156 mL 3.0389 mL
25 mM 0.0972 mL 0.4862 mL 0.9725 mL 2.4311 mL
H2O 30 mM 0.0810 mL 0.4052 mL 0.8104 mL 2.0259 mL
40 mM 0.0608 mL 0.3039 mL 0.6078 mL 1.5195 mL
50 mM 0.0486 mL 0.2431 mL 0.4862 mL 1.2156 mL
60 mM 0.0405 mL 0.2026 mL 0.4052 mL 1.0130 mL
80 mM 0.0304 mL 0.1519 mL 0.3039 mL 0.7597 mL
100 mM 0.0243 mL 0.1216 mL 0.2431 mL 0.6078 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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CRT0066101 dihydrochloride Related Classifications

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  • 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.

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CRT0066101 dihydrochloride
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