For research use only.

Catalog No.S7039

4 publications

PD168393 Chemical Structure

CAS No. 194423-15-9

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

Selleck's PD168393 has been cited by 4 publications

1 Customer Review

  • (B) Immunohistochemical staining for α-actinin and EdU showed that EGFR inhibitor (PD-168393), JNK inhibitor (sp-600125), and SP-1 inhibitor (mithramycin A) could abolish the effect of TIMP-3 siRNA in promoting cardiomyocyte proliferation. n=3 per group for Western blot. At least 2000 cells were quantified in each group. Data are shown as mean±SEM and reflect at least three independent experiments. Scale bar: 100 μm. *, P<0.05, ***, P<0.001 versus respective control.

    Theranostics, 2017, 7(3):664-676.. PD168393 purchased from Selleck.

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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.
EGFR [1]
0.70 nM
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 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:[1]
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  • Animal Models: Athymic nude mice with A431 human epidermoid carcinoma
  • Dosages: 58 mg/kg
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 73 mg/mL (197.71 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+ 40% PEG 300+5% Tween 80+50% ddH2O
For best results, use promptly after mixing.
3 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 369.22


CAS No. 194423-15-9
Storage powder
in solvent
Synonyms N/A
Smiles C=CC(=O)NC1=CC2=C(C=C1)N=CN=C2NC3=CC(=CC=C3)Br

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID