PD 168393A potent, cell-permeable, irreversible inhibitor of EGFR

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PD 168393 (CAS 194423-15-9)

PD 168393 | CAS 194423-15-9 is rated 5.0 out of 5 by 1.

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Synonym: 4-[(3-Bromophenyl)amino]-6-acrylamidoquinazoline

Application: A potent, cell-permeable, irreversible inhibitor of EGFR

CAS Number: 194423-15-9

Purity: ≥95%

Molecular Weight: 369.2

Molecular Formula: C₁₇H₁₃BrN₄O

* Refer to Certificate of Analysis for lot specific data (including water content).

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PD 168393 is a potent, irreversible, cell-permeable and selective inhibitor of EGFR (epidermal growth factor receptor). Does not inhibit any other protein kinases. PD 168393 binds to the catalytic domain of the EGFR (EGF receptor tyrosine kinase) with a 1:1 stoichiometry and alkylating Cys773.

References

Fry, D.W., et al. 1998. Proc. Natl. Acad. Sci USA 95, 12022.

Physical State :

Solid

Solubility :

Soluble in DMSO (200 mg/ml).

Storage :

Store at -20° C

Melting Point :

228.94° C (Predicted)

Boiling Point :

~571.15° C at 760 mmHg (Predicted)

Density :

~1.56 g/cm³ (Predicted)

Refractive Index :

n²⁰_D 1.74 (Predicted)

IC50 :

EGF receptor tyrosine kinase activity: IC₅₀ = 700 pM; Epidermal growth factor receptor erbB1: IC₅₀ = 0.08 nM (human); Receptor protein-tyrosine kinase erbB-2: IC₅₀ = 5.7 nM (human); Receptor protein-tyrosine kinase erbB-4: IC₅₀ = 12 nM (human); SK-BR-3: IC₅₀ = 15 nM (human)

pK Values :

pK_a: 12.19 (Predicted), pK_b: 5.33 (Predicted)

For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.

PubChem CID :

4708

MDL Number :

MFCD02179207

SMILES :

C=CC(=O)NC1=CC2=C(C=C1)N=CN=C2NC3=CC(=CC=C3)Br

Download SDS (MSDS)

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Certificate of Analysis

Catalog Number sc-222138

Lot Number

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PD 168393  Product Citations

See how others have used PD 168393. Click on the entry to view the PubMed entry .

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PMID: # 25458314  Kulkarni, NN. et al. 2015. Molecular immunology. 63: 530-9.

PMID: # notyetassignedY  Kulkarni, N.N. et al. 2014. Molecular Immunology. E-Pub ahead of print:

Citations 1 to 2 of 2 total

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Rated 5 out of 5 by ET from Sun Sun, Y. et al. (PubMed 10368634) reported that application of the EGFR inhibitor, PD 168393, caused growth termination of nasopharyngeal carcinoma cells. -SCBT Publication Review

Date published: 2015-05-17

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