Home Protein Tyrosine Kinase EGFR inhibitor PD168393 For research use only.

PD168393

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

PD168393 Chemical Structure

PD168393 Chemical Structure

CAS No. 194423-15-9

Purity & Quality Control

PD168393 Related Products

Signaling Pathway

EGFR Signaling Pathways

EGFR Signaling Pathway

Biological Activity

Description PD168393 is an irreversible EGFR inhibitor with IC50 of 0.70 nM, irreversibly alkylate Cys-773; inactive against insulin, PDGFR, FGFR and PKC.
Features Preclinical compound used in the design of CI-1033.
Targets
EGFR [1]
0.70 nM
In vitro
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. [1] 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. [2]
In Vivo
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. [1]
Animal Research Animal Models Athymic nude mice with A431 human epidermoid carcinoma
Dosages 58 mg/kg
Administration i.p.

Chemical Information & Solubility

Molecular Weight 369.22 Formula

C17H13BrN4O
CAS No. 194423-15-9 SDF Download PD168393 SDF
Smiles C=CC(=O)NC1=CC2=C(C=C1)N=CN=C2NC3=CC(=CC=C3)Br
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 74 mg/mL ( (200.42 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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