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

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

Cat. No.: HY-12013 Purity: 98.62%
Handling Instructions

PD153035 Hydrochloride (SU-5271 Hydrochloride) 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 Hydrochloride Chemical Structure

PD153035 Hydrochloride Chemical Structure

CAS No. : 183322-45-4

Size Price Stock Quantity
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
100 mg USD 504 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 3 publication(s) in Google Scholar

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Description

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

IC50 & Target

EGFR

6 pM (Ki)

EGFR

25 pM (IC50)

In Vitro

PD153035 inhibits EGF-stimulated receptor autophosphorylation in A431 human epidermoid carcinoma cells, with an IC50 of 14 nM[1]. PD153035 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 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 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].

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

In Vivo

PD153035 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 PD 153035 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].

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

Molecular Weight

396.67

Formula

C₁₆H₁₅BrClN₃O₂

CAS No.

183322-45-4

SMILES

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

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 : 5.125 mg/mL (12.92 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5210 mL 12.6049 mL 25.2099 mL
5 mM 0.5042 mL 2.5210 mL 5.0420 mL
10 mM 0.2521 mL 1.2605 mL 2.5210 mL
*Please refer to the solubility information to select the appropriate solvent.
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 (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 PD 153035 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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Keywords:

PD153035SU-5271AG1517ZM 252868PD 153035PD-153035SU5271SU 5271AG 1517AG-1517ZM252868ZM-252868EGFREpidermal growth factor receptorErbB-1HER1Inhibitorinhibitorinhibit

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Product Name:
PD153035 Hydrochloride
Cat. No.:
HY-12013
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