PD168393

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Cat No.

CEI-0881

Description

PD168393 is an irreveasible EGFR inhibitor with IC50 of 0.70 nM, irreversibly alkylate Cys-773; inactive against insulin, PDGFR, FGFR and PKC.

CAS_No

194423-15-9

Molecular Weight

369.22

Storage

2 years -20 centigrade Powder; 2 weeks 4 centigrade in DMSO; 6 months -80 centigrade in DMSO.

Targets

EGFR

IC50

0.70 nM

Molecular Formula

C17H13BrN4O

Chemical Name

2-Propenamide, N-[4-[(3-bromophenyl)amino]-6-quinazolinyl]-

Solubility

DMSO 74 mg/mL; Water <1 mg/mL; Ethanol <1 mg/mL

In vitro

PD 168393 is docked into the ATP binding pocket of EGFR TK. PD168393 completely suppresses EGF-dependent receptor autophosphorylation in A431 cells during continuous exposure, with continous suppression even after 8 hr in compound-free medium. PD168393 inhibits heregulin-induced tyrosine phosphorylation in MDA-MB-453 cells with IC50 of 5.7 nM. PD168393 is inactive against insulin, PDGF and basic FGFR TKs as well as PKC. PD168393 inhibits EGF-mediated tyrosine phosphorylation in HS-27 human fibroblasts with IC50 of 1-6 nM but has little effect on FGF- or PDGF-mediated tyrosine phosphorylation. PD168393 shows rapid and potent inhibition of Her2-induced tyrosine phosphorylation with IC50 of ~100 nM in 3T3-Her2 cells. D168393 also inhibits phosphorylation of PLCγ1/Stat1/Dok1/δ-catenin in 3T3-Her2 cells, except for Fyb.

In vivo

PD 168393 produces tumor growth inhibition of 115% in A431 human epidermoid carcinoma xenograft in nude mice, with 50% reduced phosphotyrosine content of EGFR. PD 168393 also shows a low plasma concentration.

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