PD168393

Catalog No.S7039 Batch:S703901

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Technical Data

Formula

C17H13BrN4O
Molecular Weight 369.22 CAS No. 194423-15-9
Solubility (25°C)* In vitro DMSO 74 mg/mL (200.42 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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.
Targets
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]
Features Preclinical compound used in the design of CI-1033.

Protocol (from reference)

Animal Study:[1]
  • Animal Models

    Athymic nude mice with A431 human epidermoid carcinoma

  • Dosages

    58 mg/kg

  • Administration

    i.p.

Customer Product Validation

Data from [Data independently produced by , , Theranostics, 2017, 7(3):664-676.]

Selleck's PD168393 has been cited by 5 publications

The EGF/EGFR axis and its downstream signaling pathways regulate the motility and proliferation of cultured oral keratinocytes [ FEBS Open Bio, 2023, 10.1002/2211-5463.13653] PubMed: 37243482
Schwann cell precursors generate sympathoadrenal system during zebrafish development [ J Neurosci Res, 2021, 10.1002/jnr.24909] PubMed: 34184294
Cbfα1 hinders autophagy by DSPP upregulation in odontoblast differentiation. [ Int J Biochem Cell Biol, 2019, 115:105578] PubMed: 31374250
miR-17-3p Contributes to Exercise-Induced Cardiac Growth and Protects against Myocardial Ischemia-Reperfusion Injury. [Shi J, et al. Theranostics, 2017, 7(3):664-676] PubMed: 28255358
[ Oncotarget, 2016, ] PubMed: 27322144

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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