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K-Ras-PDEδ-IN-1

This product is for research use only, not for human use. We do not sell to patients.

K-Ras-PDEδ-IN-1
For small sizes, please check our retail website as below: www.invivochem.com
Size Price Stock
100mg$3250Check With Us
200mg$4875Check With Us
500mg$8225Check With Us
email: [email protected]        [email protected]

Cat #: V2209 CAS #: 1841464-21-8 Purity ≥ 98%

Description: K-Ras-PDEδ-IN-1 is a novel and potent competitive K-Ras-PDEδ inhibitor.

References: Sandip Murarka, et al. Development of Pyridazinone Chemotypes Targeting the PDEδ Prenyl Binding Site. Chemistry. 2017 May 2;23(25):6083-6093.

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Molecular Weight (MW)447.50
Molecular FormulaC25H26FN5O2
CAS No.1841464-21-8
SMILES Code O=C(NCCC1=CC=C(F)C=C1)CCCN2N=C(C)C3=CN(C4=CC=C(C)C=C4)N=C3C2=O
SynonymsK-Ras-PDEδ-IN-1
ProtocolIn VitroK-Ras-PDEδ-IN-1 exhibits an IC50 value of 12.3 μM in PaTu8902/Panc1 CTG assay.
In VivoK-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. 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.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Preparing Stock Solutions
Solvent volume to be added Mass (the weight of a compound)
Mother liquor concentration 1mg5mg10mg20mg
1mM2.2346 mL11.1732 mL22.3464 mL44.6927 mL
5mM0.4469 mL2.2346 mL4.4693 mL8.9385 mL
10mM0.2235 mL1.1173 mL2.2346 mL4.4693 mL
20mM0.1117 mL0.5587 mL1.1173 mL2.2346 mL
Quality Control Documentation
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
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The dilution calculator equation
Concentration(start) × Volume(start) = Concentration(final) × Volume(final)

This equation is commonly abbreviated as: C1 V1 = C2 V2

Concentration(start)
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Step One: Enter information below
Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals
Step Two: Enter the in vivo formulation
%DMSO + % + %Tween 80 + %ddH2O
Calculation Results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in µL DMSO(Master liquid concentration mg/mL) ,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation: Take µL DMSO master liquid, next add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH2O,mix and clarify.
Note:
  • (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
  • (2) Be sure to add the solvent(s) in order.