1. Apoptosis
  2. PKD
  3. CRT0066101 dihydrochloride

CRT0066101 dihydrochloride 

Cat. No.: HY-15698A Purity: 99.53%
Handling Instructions

CRT0066101 dihydrochloride is a potent and specific PKD inhibitor with IC50 values of 1, 2.5 and 2 nM for PKD1, 2, and 3 respectively.

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

CRT0066101 dihydrochloride Chemical Structure

CRT0066101 dihydrochloride Chemical Structure

CAS No. : 1883545-60-5

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 99 In-stock
Estimated Time of Arrival: December 31
5 mg USD 90 In-stock
Estimated Time of Arrival: December 31
10 mg USD 168 In-stock
Estimated Time of Arrival: December 31
25 mg USD 360 In-stock
Estimated Time of Arrival: December 31
50 mg USD 672 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

CRT0066101 dihydrochloride is a potent and specific PKD inhibitor with IC50 values of 1, 2.5 and 2 nM for PKD1, 2, and 3 respectively.

IC50 & Target[1]

PKD1

1 nM (IC50)

PKD3

2 nM (IC50)

PKD2

2.5 nM (IC50)

In Vitro

CRT0066101 specifically blocks PKD1/2 activity and does not suppress PKCα/PKCβ/PKCε activity in multiple cancer cell types including A549 (lung) and MiaPaCa-2 (pancreas). CRT0066101 significantly inhibits Panc-1 cell proliferation with an IC50 value of 1 µM. Treatment with 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 has a modest effect in Capan-2 cells. CRT0066101 (5 µM) blocks both the basal and NT-induced pS916-PKD1/2 (activated PKD1/2) in Panc-1 and Panc-28 cells. CRT0066101 reduces PKD-dependent NF-κB activation and NF-κB-dependent gene expressions in Panc-1[1].

In Vivo

Optimal therapeutic concentrations (8 µM) of CRT0066101 are detectable 6 h after oral administration of this drug. CRT0066101 given orally (80 mg/kg/day) for 28 days significantly abrogates PaCa growth in Panc-1 subcutaneous xenograft model. Activated PKD1/2 expression in the treated tumor-explants is significantly inhibited with peak tumor concentration (12 µM) of CRT0066101 achieved within 2 h after oral administration. Further, CRT0066101 given orally (80 mg/kg/day) for 21 days in Panc-1 orthotopic model potently blocks tumor growth in vivo. CRT0066101 significantly reduces Ki-67+ proliferation index, increases TUNEL+ apoptotic cells (p<0.05), and abrogates expression of NF-κB-dependent proteins including cyclin D1, survivin, and cIAP-1[1].

Molecular Weight

411.33

Formula

C₁₈H₂₄Cl₂N₆O

CAS No.

1883545-60-5

SMILES

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

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: 

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

DMSO : ≥ 25 mg/mL (60.78 mM)

*"≥" means soluble, but saturation unknown.

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
10 mM 0.2431 mL 1.2156 mL 2.4311 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

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

    Solubility: ≥ 1 mg/mL (2.43 mM); Clear solution

  • 2.

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

    Solubility: ≥ 1 mg/mL (2.43 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 1 mg/mL (2.43 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Animal Administration
[1]

Mice: Nineteen days after implantation of Panc-1 cells, tumor areas are, on average 0.3 cm2 and are randomized into the following groups (n=8 mice per group): (a) vehicle (control) 5% dextrose administered by oral gavage once daily and (b) 80 mg/kg CRT0066101 dissolved in 5% dextrose administered by oral gavage once daily. Tumors are measured in 2 dimensions every 2 to 3 days by calipers and area is calculated by multiplying length by width. Therapy is given until tumors reached their designated size limits (1.44 cm2) or until day 24 in CRT0066101 treated group. Final tumor areas are compared among groups using a Student's t test and Fisher’s exact test with p<0.05[1].

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

References
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Keywords:

CRT0066101CRT 0066101CRT-0066101PKDProtein kinase DInhibitorinhibitorinhibit

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CRT0066101 dihydrochloride
Cat. No.:
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