PD168393

Catalog No.S7039

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

Price Stock Quantity  
USD 810 In stock
USD 170 In stock
Bulk Inquiry

Massive Discount Available

Free Overnight Delivery on all orders over $ 500.

PD168393 Chemical Structure

PD168393 Chemical Structure
Molecular Weight: 369.22

Validation & Quality Control

Quality Control & MSDS

Product Information

  • Compare EGFR Inhibitors
    Compare EGFR Products
  • Research Area
  • Inhibition Profile

Product Description

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] Insulin Receptor [1] PDGFR [1] FGFR [1] PKC [1]
IC50 0.70 nM >50 μM >50 μM >50 μM >50 μM
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(Only for Reference)

Kinase Assay: [1]

Enzyme Assays The enzyme assay is performed in 96-well filte plates. The total volume is 0.1 mL containing 20 mM HEPES, pH 7.4, 50 μM sodium vanadate, 40 mM magnesium chloride, 10 μM ATP containing 0.5 μCi of [32P]ATP, 20 μg of polyglutamic acid/tyrosine, 1 ng of EGF receptor tyrosine kinase, and appropriate dilutions of inhibitor and/or ATP. All components except the ATP are added to the well, and the plate is incubated with shaking for 10 min at 25 °C. The reaction is started by adding [32P]ATP, and the plate is incubated with shaking at 25 °C for 10 min. The reaction is terminated by the addition of 0.1 mL of 20% TCA, and the plate is kept at 4 °C for at least 15 min to allow the substrate to precipitate. The wells are then washed five times with 0.125 mL of 10% TCA, and [32P] incorporation is determined with a Wallac beta plate counter. To assess the type of inhibition, kinetic data are fitted by nonlinear regression computer programs.

Animal Study: [1]

Animal Models Athymic nude mice with A431 human epidermoid carcinoma
Formulation 4% dimethylacetamide in aqueous 50 mM sodium lactate buffer (pH 4)
Dosages 58 mg/kg
Administration i.p.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
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.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[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.

Chemical Information

Download PD168393 SDF
Molecular Weight (MW) 369.22
Formula

C17H13BrN4O

CAS No. 194423-15-9
Storage 3 years -20℃powder
2 years -80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 74 mg/mL (200.42 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo 30% PEG400+0.5% Tween80+5% propylene glycol 10 mg/mL
* <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.
Chemical Name 2-Propenamide, N-[4-[(3-bromophenyl)amino]-6-quinazolinyl]-

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

* Indicates a Required Field

Related EGFR Products

  • Erlotinib

    Erlotinib is an EGFR inhibitor with IC50 of 2 nM, >1000-fold more sensitive for EGFR than human c-Src or v-Abl.

  • Afatinib (BIBW2992) Dimaleate

    Afatinib (BIBW2992) Dimaleate irreversibly inhibits EGFR/HER2 including EGFR(wt), EGFR(L858R), EGFR(L858R/T790M) and HER2 with IC50 of 0.5 nM, 0.4 nM, 10 nM and 14 nM, respectively; 100-fold more active against Gefitinib-resistant L858R-T790M EGFR mutant.

  • Poziotinib (HM781-36B)

    Poziotinib (HM781-36B) is an irreversible pan-HER inhibitor with IC50 of 3.2 nM, 5.3 nM and 23.5 nM for HER1, HER2, and HER4, respectively. Phase 2.

  • Gefitinib (ZD1839)

    Gefitinib (ZD-1839) is an EGFR inhibitor for Tyr1173, Tyr992, Tyr1173 and Tyr992 in the NR6wtEGFR and NR6W cells with IC50 of 37 nM, 37nM, 26 nM and 57 nM, respectively.

    Features:A potent EGFR tyrosine kinase inhibitor.

  • Erlotinib HCl (OSI-744)

    Erlotinib HCl (OSI-744) is an EGFR inhibitor with IC50 of 2 nM in cell-free assays, >1000-fold more sensitive for EGFR than human c-Src or v-Abl.

  • Afatinib (BIBW2992)

    Afatinib (BIBW2992) irreversibly inhibits EGFR/HER2 including EGFR(wt), EGFR(L858R), EGFR(L858R/T790M) and HER2 with IC50 of 0.5 nM, 0.4 nM, 10 nM and 14 nM in cell-free assays, respectively; 100-fold more active against Gefitinib-resistant L858R-T790M EGFR mutant.

  • Osimertinib (AZD9291)

    Osimertinib (AZD9291) is an oral, irreversible, and mutant-selective EGFR inhibitor with IC50 of 12.92, 11.44 and 493.8 nM for Exon 19 deletion EGFR, L858R/T790M EGFR, and WT EGFR in LoVo cells, respectively. Phase 3.

  • Lapatinib

    Lapatinib, used in the form of Lapatinib Ditosylate, is a potent EGFR and ErbB2 inhibitor with IC50 of 10.8 and 9.2 nM in cell-free assays, respectively.

  • AG-490 (Tyrphostin B42)

    AG-490 (Tyrphostin B42) is an inhibitor of EGFR with IC50 of 0.1 μM in cell-free assays, 135-fold more selective for EGFR versus ErbB2, also inhibits JAK2 with no activity to Lck, Lyn, Btk, Syk and Src.

  • Rociletinib (CO-1686, AVL-301)

    Rociletinib (CO-1686, AVL-301) is an irreversible, mutant-selective EGFR inhibitor with Ki of 21.5 nM and 303.3 nM for EGFRL858R/T790M and EGFRWT in cell-free assays, respectively. Phase 2.

Recently Viewed Items

Tags: buy PD168393 | PD168393 supplier | purchase PD168393 | PD168393 cost | PD168393 manufacturer | order PD168393 | PD168393 distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Contact Us