1. Protein Tyrosine Kinase/RTK
    JAK/STAT Signaling
    Autophagy
    Apoptosis
  2. EGFR
    Autophagy
    Apoptosis
  3. PD168393

PD168393 

Cat. No.: HY-13896 Purity: 98.87%
Handling Instructions

PD168393 is a potent, selective and cell-permeable inhibitor of EGFR tyrosine kinase and ErbB2. PD168393 irreversiblely inactivates EGF receptor ( IC50=0.7 nM) and is inactive against insulin receptor, PDGFR, FGFR and PKC.

For research use only. We do not sell to patients.

PD168393 Chemical Structure

PD168393 Chemical Structure

CAS No. : 194423-15-9

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Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 57 In-stock
Estimated Time of Arrival: December 31
2 mg USD 50 In-stock
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5 mg USD 70 In-stock
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10 mg USD 110 In-stock
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25 mg USD 190 In-stock
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50 mg USD 280 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

PD168393 is a potent, selective and cell-permeable inhibitor of EGFR tyrosine kinase and ErbB2. PD168393 irreversiblely inactivates EGF receptor ( IC50=0.7 nM) and is inactive against insulin receptor, PDGFR, FGFR and PKC[1].

IC50 & Target[1]

EGFR

0.7 nM (IC50)

In Vitro

PD168393 inhibits ligand-dependent receptor phosphorylation and inhibits EGF-induced tyrosine phosphorylation in A431 cells and Heregulin-induced tyrosine phosphorylation in MDA-MB-453 cells with IC50 values of 4.3  nM and 5.7  nM, respectively[1].

In Vivo

PD168393 (intraperitoneal injection; 58 mg/kg; once daily; days 10-14, 17-21, and 24-28) is effective in vivo, and produces tumor growth inhibition of 115% after 15 days’ treatment in human epidermoid carcinoma xenografts in mice[1].

Animal Model: A431 human epidermoid carcinoma grown as a xenograft in nude mice[1]
Dosage: 58 mg/kg
Administration: Intraperitoneal injection; 58 mg/kg; once daily; days 10-14, 17-21, and 24-28
Result: Suppressed the growth of human epidermoid carcinoma xenografts.
Molecular Weight

369.22

Formula

C₁₇H₁₃BrN₄O

CAS No.

194423-15-9

SMILES

C=CC(NC1=CC2=C(NC3=CC=CC(Br)=C3)N=CN=C2C=C1)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 30 mg/mL (81.25 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7084 mL 13.5421 mL 27.0841 mL
5 mM 0.5417 mL 2.7084 mL 5.4168 mL
10 mM 0.2708 mL 1.3542 mL 2.7084 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.77 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

PD168393PD 168393PD-168393EGFRAutophagyApoptosisEpidermal growth factor receptorErbB-1HER1MDA-MB-453tumor epidermoid carcinomaPDGFRFGFRInhibitorinhibitorinhibit

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PD168393
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