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PD168393

Cat. No. M2916
PD168393 Structure
Size Price Availability Quantity
1mg USD 100 In stock
5mg USD 180 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

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

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 369.22
Formula C17H13BrN4O
CAS Number 194423-15-9
Purity >99%
Solubility DMSO 70 mg/mL
Storage at -20°C
Customer Product Validations & Biological Datas
Source Neuro Oncol (2012). Figure 1. PD168393
Method apoptosis assay
Cell Lines MPNST cells
Concentrations 2 μM
Incubation Time 24–48 h
Results Taken together, these data indicate that PD168393-induced block in erbB signaling is largely cytostatic and has no effect on MPNST cell apoptosis.
Rating
References

Phosphoproteomic analysis of Her2/neu signaling and inhibition.
Bose R, et al. Proc Natl Acad Sci U S A. 2006 Jun 27;103(26):9773-8. PMID: 16785428.

Specific, irreversible inactivation of the epidermal growth factor receptor and erbB2, by a new class of tyrosine kinase inhibitor.
Fry DW, et al. Proc Natl Acad Sci U S A. 1998 Sep 29;95(20):12022-7. PMID: 9751783.

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  Catalog
Abmole Inhibitor Catalog 2017




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