1. Protein Tyrosine Kinase/RTK
    JAK/STAT Signaling
  2. EGFR
  3. PD153035

PD153035 (Synonyms: SU-5271; AG1517; ZM 252868)

Cat. No.: HY-14346 Purity: 98.66%
Handling Instructions

PD153035 (SU-5271; AG1517; ZM 252868) is a potent EGFR inhibitor with Ki and IC50 of 6 and 25 pM, respectively.

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

PD153035 Chemical Structure

PD153035 Chemical Structure

CAS No. : 153436-54-5

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10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
5 mg USD 60 In-stock
Estimated Time of Arrival: December 31
10 mg USD 78 In-stock
Estimated Time of Arrival: December 31
50 mg USD 298 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 2 publication(s) in Google Scholar

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Description

PD153035 (SU-5271; AG1517; ZM 252868) is a potent EGFR inhibitor with Ki and IC50 of 6 and 25 pM, respectively.

IC50 & Target[1]

EGFR

6 pM (Ki)

EGFR

25 pM (IC50)

In Vitro

PD153035 (SU 5271) inhibits EGF-stimulated receptor autophosphorylation in A431 human epidermoid carcinoma cells, with an IC50 of 14 nM[1]. PD153035 (SU 5271) has little effect on PDGFR, FGFR, CSF-1 receptor, the insulin receptor, or on src tyrosine kinases at concentrations as high as 50 μM. PD153035 (SU 5271) rapidly suppresses autophosphorylation of the EGF receptor at low nanomolar concentrations in fibroblasts or in human epidermoid carcinoma cells and selectively blocks EGF-mediated cellular processes including mitogenesis, early gene expression, and oncogenic transformation[2]. PD153035 (SU 5271) causes a dose-dependent growth inhibition of EGF receptor-positive cell lines, beginning at less than micromolar concentrations, and the IC50 is less than 1 pM in most cases[3].

In Vivo

PD153035 (SU 5271) levels in the plasma and tumor rise to 50 and 22 μM within 15 minutes following a single i.p. dose of 80 mg/kg. While the plasma levels of PD153035 (SU 5271) falls below 1 μM by 3 hours, in the tumors it remains at micromolar concentrations for at least 12 hours. The tyrosine phosphorylation of the EGF receptor is rapidly suppressed by 80-90% in the tumors[4].

Molecular Weight

360.21

Formula

C₁₆H₁₄BrN₃O₂

CAS No.

153436-54-5

SMILES

COC1=C(C=C(C2=C1)N=CN=C2NC3=CC(Br)=CC=C3)OC

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 : 33.33 mg/mL (92.53 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7762 mL 13.8808 mL 27.7616 mL
5 mM 0.5552 mL 2.7762 mL 5.5523 mL
10 mM 0.2776 mL 1.3881 mL 2.7762 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.94 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Cell Assay
[3]

Different EGF receptor-overexpressing cell lines (A43 1, Difi, MDA-MB-468, MDA-MB-231, DU145, SiHa, C4i, and MEl 80) are treated with PD153035 at increasing concentrations of 0.125-2.5 p.M. Growth inhibitory effect in monolayer cell culture is assessed[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[3]

Mice: Mice are injected with PD153035 (SU 5271) (80 mg/kg) or vehicle and rumors are excised at 20 minutes and 180 minutes and extracts are prepared. Two mice are used for each time point and the experiment is repeated four times. Within each of the four experiments ANOVA is used to compare the inhibition by PD153035 (SU 5271) of the EGF-stimulation[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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PD153035
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