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.
Product information
CAS Number: 1841464-21-8
Molecular Weight: 447.50
Formula: C25H26FN5O2
Chemical Name: N-[2-(4-fluorophenyl)ethyl]-4-[4-methyl-2-(4-methylphenyl)-7-oxo-2H,6H,7H-pyrazolo[3,4-d]pyridazin-6-yl]butanamide
Smiles: CC1C=CC(=CC=1)N1C=C2C(=N1)C(=O)N(CCCC(=O)NCCC1=CC=C(F)C=C1)N=C2C
InChiKey: RRELLHHWESTKAK-UHFFFAOYSA-N
InChi: InChI=1S/C25H26FN5O2/c1-17-5-11-21(12-6-17)31-16-22-18(2)28-30(25(33)24(22)29-31)15-3-4-23(32)27-14-13-19-7-9-20(26)10-8-19/h5-12,16H,3-4,13-15H2,1-2H3,(H,27,32)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 12.5 mg/mL (27.93 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
K-Ras-PDEδ-IN-1 exhibits an IC50 value of 12.3 μM in PaTu8902/Panc1 CTG assay.
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. 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.
Products are for research use only. Not for human use.
Payment & Security
Your payment information is processed securely. We do not store credit card details nor have access to your credit card information.