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PD168393

Catalog No. T6932   CAS 194423-15-9
Synonyms: Autophagy, EGFR, ErbB-1, HER1, PD 168393, PD168393, Apoptosis, PDGFR, Epidermal growth factor receptor, tumor, PD-168393, epidermoid carcinoma, Inhibitor, FGFR, inhibit

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

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PD168393, CAS 194423-15-9
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Purity: 98%
Biological Description
Chemical Properties
Storage & Solubility Information
Description PD168393 is an irreversible EGFR inhibitor (IC50: 0.70 nM), irreversibly alkylate Cys-773; inactive against PKC, FGFR, PDGFR, and insulin.
Targets&IC50 EGFR: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]
Kinase Assay The effects of VU0364770 on rat mGlu1 and mGlu5 are assessed by using calcium mobilization and measuring the glutamate concentration-response relationship in the presence and absence of 10 μM VU0364770. Using a double-addition protocol, VU0364770 is added to the cells, followed 2.5 min later by a full concentration-response of glutamate. Shifts of the concentration-response relationship are used to assess potential potentiator (left shift of more than 2-fold) or antagonist (right shift of more than 2-fold or depression of the maximum response by at least 75%) activity of VU0364770. Compounds are further assessed for mGlu5 antagonist activity by performing a full concentration-response curve, starting at 30 μM and serially diluted it by using 1:3 dilutions, in the presence of an EC80 concentration of glutamate[1].
Synonyms Autophagy, EGFR, ErbB-1, HER1, PD 168393, PD168393, Apoptosis, PDGFR, Epidermal growth factor receptor, tumor, PD-168393, epidermoid carcinoma, Inhibitor, FGFR, inhibit
Molecular Weight 369.222
Formula C17H13BrN4O
CAS No. 194423-15-9

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

Ethanol: <1 mg/mL

H2O: <1 mg/mL

DMSO: 68 mg/mL (184.2 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Citations

References and Literature
1. Fry W, et al. Proc Natl Acad Sci U S A. 1998, 95(20), 12022-12027. 2. Bose R, et al. Proc Natl Acad Sci U S A, 2006, 103(26), 9773-9778.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Compound Library Preclinical Compound Library Autophagy Compound Library Anti-Lung Cancer Compound Library GPCR Compound Library Glycometabolism Compound Library Anti-Cancer Metabolism Compound Library Anti-Obesity Compound Library Anti-Pancreatic Cancer Compound Library Inhibitor Library

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