Description
AZ12672857 is an orally active inhibitor of EphB4 (IC50=1.3 nM) and Src kinases. AZ12672857 shows good inhibition of proliferation of c-Src transfected 3T3 cells (IC50=2 nM) as well as autophosphorylation of EphB4 in transfected CHO-K1 cells (IC50=9 nM).
Product information
CAS Number: 945396-55-4
Molecular Weight: 494.63
Formula: C26H38N8O2
Chemical Name: N2-[3,5-bis(morpholin-4-yl)phenyl]-N4-methyl-N4-(octahydro-1H-indazol-4-yl)pyrimidine-2,4-diamine
Smiles: CN(C1CCCC2NNCC21)C1=CC=NC(NC2C=C(C=C(C=2)N2CCOCC2)N2CCOCC2)=N1
InChiKey: GNLBYJJNAFTWTI-UHFFFAOYSA-N
InChi: InChI=1S/C26H38N8O2/c1-32(24-4-2-3-23-22(24)18-28-31-23)25-5-6-27-26(30-25)29-19-15-20(33-7-11-35-12-8-33)17-21(16-19)34-9-13-36-14-10-34/h5-6,15-17,22-24,28,31H,2-4,7-14,18H2,1H3,(H,27,29,30)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 25 mg/mL (51.38 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:
AZ12672857 shows only modest inhibition of CYP P450 (IC50=5 μM against 2C9 and 3A4, >10 μM against 1A4, 2D6 and 2C19). AZ12672857 inhibits p-KDR in HUVEC with an IC50 of 240 nM and inhibits p-PDGFR-βin MG63 cell line with an IC50 of 58 nM.
Products are for research use only. Not for human use.
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