1. Metabolic Enzyme/Protease
  2. Phosphodiesterase (PDE)
  3. K-Ras-PDEδ-IN-1

K-Ras-PDEδ-IN-1 

Cat. No.: HY-115555 Purity: 99.33%
Handling Instructions

K-Ras-PDEδ-IN-1 is a novel and potent competitive K-Ras-PDEδ inhibitor. K-Ras-PDEδ-IN-1 binds to the farnesyl binding pocket of PDEδ with a low nanomolar Kd of 8 nM.

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

K-Ras-PDEδ-IN-1 Chemical Structure

K-Ras-PDEδ-IN-1 Chemical Structure

CAS No. : 1841464-21-8

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 330 In-stock
Estimated Time of Arrival: December 31
5 mg USD 300 In-stock
Estimated Time of Arrival: December 31
10 mg USD 480 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1400 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2000 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

K-Ras-PDEδ-IN-1 is a novel and potent competitive K-Ras-PDEδ inhibitor. K-Ras-PDEδ-IN-1 binds to the farnesyl binding pocket of PDEδ with a low nanomolar Kd of 8 nM[1].

IC50 & Target[1]

PDE4

8.3 nM (Kd)

In Vitro

K-Ras-PDEδ-IN-1 exhibits an IC50 value of 12.3 μM in PaTu8902/Panc1 CTG assay[1].

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

In Vivo

K-Ras-PDEδ-IN-1 (oral or intraperitoneal injection; 10 mg/kg; single dose) is in different vehicles (A=5% Tween-80, 50% NaCl, 45% H2O; B=20% DMSO, 80% PEG200; C=15% DMSO, 9.5% Cremophor EL/EtOH (1:1), 75.5 % H2O) for oral and intraperitoneal (IP) administration.whereas only very low compound levels are found in plasma after oral dosage, but significantly higher plasma concentrations are found after IP administration in vehicle A, B or C at 10 mg kg[1].
K-Ras-PDEδ-IN-1 (intravenous injection; 3 mg kg; single dose; 24 hours) shows a significant increase of the plasma exposure as well as the terminal half-life (t1/2=0.4 hours)when compares to compound 93,exhibits a t1/2, CO, AUC0-tz, AUC0.inf-obs, Clobs, and Vss0-inf-obs values of 4.1 hours, 2790.9 ng/ml, 1646.4 h.ng/ml, 1662.5 h.ng/ml, 1.8 L/h/kg, 5.9 l/kg[1].

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

Molecular Weight

447.50

Formula

C₂₅H₂₆FN₅O₂

CAS No.

1841464-21-8

SMILES

O=C(NCCC1=CC=C(F)C=C1)CCCN2N=C(C)C3=CN(C4=CC=C(C)C=C4)N=C3C2=O

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 : 12.5 mg/mL (27.93 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2346 mL 11.1732 mL 22.3464 mL
5 mM 0.4469 mL 2.2346 mL 4.4693 mL
10 mM 0.2235 mL 1.1173 mL 2.2346 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: 1.25 mg/mL (2.79 mM); Suspended solution; Need ultrasonic

*All of the co-solvents are provided by MCE.
References
  • 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.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

K-Ras-PDEδ-IN-1Phosphodiesterase (PDE)pyrazolopyridazinone-basedK-Ras-PDEδcancerPDEδInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email address *

Phone number *

 

Organization name *

Department *

 

Requested quantity *

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
K-Ras-PDEδ-IN-1
Cat. No.:
HY-115555
Quantity:
MCE Japan Authorized Agent: