PD168393

Catalog No.S7039 Batch:S703902

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Technical Data

Formula

C17H13BrN4O
Molecular Weight 369.22 CAS No. 194423-15-9
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.)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O

Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.

 3.000mg/ml (8.13mM) Taking the 1 mL working solution as an example, add 50 μL 60 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <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.)

Preparing Stock Solutions

Biological Activity

Description PD168393 is an irreversible EGFR inhibitor with IC50 of 0.70 nM, irreversibly alkylating Cys-773; this compound is inactive against insulin, PDGFR, FGFR and PKC.
Targets
EGFR
0.70 nM
In vitro PD 168393 is docked into the ATP binding pocket of EGFR TK. This compound completely suppresses EGF-dependent receptor autophosphorylation in A431 cells during continuous exposure, with continuous suppression even after 8 hr in compound-free medium. It inhibits heregulin-induced tyrosine phosphorylation in MDA-MB-453 cells with IC50 of 5.7 nM. This chemical is inactive against insulin, PDGF and basic FGFR TKs as well as PKC. It 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. This compound shows rapid and potent inhibition of Her2-induced tyrosine phosphorylation with IC50 of ~100 nM in 3T3-Her2 cells. It also inhibits phosphorylation of PLCγ1/Stat1/Dok1/δ-catenin in 3T3-Her2 cells, except for Fyb.
In Vivo PD 168393 produces tumour growth inhibition of 115% in A431 human epidermoid carcinoma xenografts in nude mice, with 50% reduced phosphotyrosine content of EGFR. This compound also shows a low plasma concentration.
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.

References

  • http://www.ncbi.nlm.nih.gov/pmc/articles/PMC21758/
  • https://pubmed.ncbi.nlm.nih.gov/16785428/

Customer Product Validation

(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.

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

Sellecks PD168393 Has Been Cited by 6 Publications

The interferon-rich skin environment regulates Langerhans cell ADAM17 to promote photosensitivity in lupus [ Elife, 2024, 13e85914] PubMed: 38860651
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

RETURN POLICY
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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.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.