Description
DDR1-IN-4 (Compound 2.45) is a selective and potent Discoidin Domain Receptor 1 (DDR1) autophosphorylation inhibitor, with IC50 values of 29 nM and 1.9 μM for DDR1 and DDR2, respectively.
Product information
CAS Number: 2125676-13-1
Molecular Weight: 565.34
Formula: C23H20BrF3N6O3
Chemical Name: 2-(4-bromo-2-oxo-1'-{1H-pyrazolo[4,3-b]pyridine-5-carbonyl}-1,2-dihydrospiro[indole-3,4'-piperidin]-1-yl)-N-(2,2,2-trifluoroethyl)acetamide
Smiles: O=C1N(CC(=O)NCC(F)(F)F)C2=CC=CC(Br)=C2C21CCN(CC2)C(=O)C1=CC=C2NN=CC2=N1
InChiKey: UXEXYURPAPXPSR-UHFFFAOYSA-N
InChi: InChI=1S/C23H20BrF3N6O3/c24-13-2-1-3-17-19(13)22(21(36)33(17)11-18(34)28-12-23(25,26)27)6-8-32(9-7-22)20(35)15-5-4-14-16(30-15)10-29-31-14/h1-5,10H,6-9,11-12H2,(H,28,34)(H,29,31)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
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:
DDR1-IN-4 (Compound 2.45) shows a clear dose-dependent inhibition of DDR1 phosphorylation in HT1080 cells overexpressing DDR1, with greater than 70% inhibition of phosphorylation at a concentration of 1 μM, and retaining selectivity over inhibition of DDR2.
In Vivo:
DDR1-IN-4 (Compound 2.45, ip, 90 mg/kg) preserves renal function and reduces tissue damage in Col4a3–/– mice (the preclinical mouse model of Alport syndrome) when employing a therapeutic dosing regime, indicating the real therapeutic value of selectively inhibiting DDR1 phosphorylation in vivo.
Products are for research use only. Not for human use.
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