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Pelitinib

Chemical Structure : Pelitinib

CAS No.: 257933-82-7

Pelitinib (EKB-569;WAY-EKB 569;EKB569;EKB 569)

Catalog No.: PC-45812Not For Human Use, Lab Use Only.

Pelitinib (EKB-569, WAY-EKB 569) is a potent, selective, orally active, irreversible inhibitor of EGFR with IC50 of 80 nM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Pelitinib (EKB-569, WAY-EKB 569) is a potent, selective, orally active, irreversible inhibitor of EGFR with IC50 of 80 nM.
Pelitinib (EKB-569, WAY-EKB 569) inhibits autophosphorylation of the cytoplasmic domain of HER-2 with IC50 of 1.23 uM.
Pelitinib (EKB-569, WAY-EKB 569) shows 1-3 orders of magnitude higher IC50 value for Src, Cdk4, c-Met, Raf, and MEK/ERK.
Pelitinib (EKB-569, WAY-EKB 569) inhibits proliferation in NHEK, A431, and MDA-468 cells (IC50= 61, 125, and 260 nM, respectively).
Pelitinib (EKB-569, WAY-EKB 569) potently inhibits the EGFR phosphorylation in A431 xenografts, suppresses tumorigenesis in APCMin/+ mice.

Physicochemical Properties

M.Wt 467.9231
Formula C24H23ClFN5O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: 16 mg/mL

Chemical Name/SMILES

2-Butenamide, N-[4-[(3-chloro-4-fluorophenyl)amino]-3-cyano-7-ethoxy-6-quinolinyl]-4-(dimethylamino)-, (2E)-

References

1. Wissner A, et al. J Med Chem. 2003 Jan 2;46(1):49-63.

2. Nunes M, et al. Mol Cancer Ther. 2004 Jan;3(1):21-7.

3. Torrance CJ, et al. Nat Med. 2000 Sep;6(9):1024-8.

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