| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 500mg |
|
||
| Other Sizes |
|
Purity: ≥98%
PD153035 is reported to be a novel, potent, specific, and ATP competitive inhibitor of EGFR (Epidermal growth factor receptor) tyrosine kinase with Ki and IC50 of 5.2 pM and 29 pM in cell-free assays, and to a lesser degree, of the closely related HER2/neu receptor; PD153035 inhibits EGF-dependent EGFR phosphorylation in a variety of human cancer cell lines over-expressing EGFRs, which include A431, Difi, DU145, MDA-MB-468, ME180 and C4i, with IC50 of 0.22 μM, 0.3 μM, 0.4 μM, 0.68 μM, 0.95 μM and 2.5 μM respectively. In addition, PD153035 could reverse ABCG2-mediated MDR in vitro (in human NSCLC and transfected cells overexpressing ABCG2) and in vivo. One of the major mediators of multidrug resistance (MDR) in non-small cell lung cancer (NSCLC) is the overexpression of ATP-binding cassette subfamily G member 2 (ABCG2). Therefore, PD153035 may be a promising therapeutic strategy for NSCLC overexpressing ABCG2.
| ln Vitro |
With an IC50 of 14 nM, PD153035 (SU 5271) inhibits EGF-stimulated receptor autophosphorylation in human epidermoid carcinoma A431 cells[1]. Even at 50 μM, PD153035 (SU 5271) has minimal effect on src tyrosine kinases, insulin receptor, PDGFR, FGFR, CSF-1 receptor, or CSF-1 receptor. In fibroblasts or human epidermoid carcinoma cells, PD153035 (SU 5271) quickly suppresses autophosphorylation of the EGF receptor at low nanomolar doses and specifically prevents EGF-mediated cellular activities such as mitogenesis, early gene expression, and oncogenic transformation[2]. EGF receptor-positive cell lines are subjected to a dose-dependent growth inhibition by PD153035 (SU 5271), which starts at less than micromolar concentrations and typically has an IC50 of less than 1 pM[3].
|
||
|---|---|---|---|
| ln Vivo |
After a single intraperitoneal (i.p.) injection of 80 mg/kg, PD153035 (SU 5271) levels in the tumor and plasma rise to 22 μM and 50 μM after 15 minutes as well. In tumors, PD153035 (SU 5271) remains at micromolar concentrations for at least 12 hours, even though its plasma levels drop below 1 μM after three hours. Tumors quickly decrease the tyrosine phosphorylation of the EGF receptor by 80–90%[4].
|
||
| Animal Protocol |
|
||
| References |
[1]. Bridges AJ, et al. Tyrosine kinase inhibitors. 8. An unusually steep structure-activity relationship for analogues of 4-(3-bromoanilino)-6,7-dimethoxyquinazoline (PD 153035), a potent inhibitor of the epidermal growth factor receptor. J Med Chem. 1996 Jan
[2]. Fry DW, et al. A specific inhibitor of the epidermal growth factor receptor tyrosine kinase. Science. 1994 Aug 19;265(5175):1093-5. [3]. Bos M, et al. PD153035, a tyrosine kinase inhibitor, prevents epidermal growth factor receptoractivation and inhibits growth of cancer cells in a receptor number-dependent manner. Clin Cancer Res. 1997 Nov;3(11):2099-106. [4]. Kunkel MW, et al. Inhibition of the epidermal growth factor receptor tyrosine kinase by PD153035 in human A431 tumors in athymic nude mice. Invest New Drugs. 1996;13(4):295-302 |
| Molecular Formula |
C16H14BRN3O2
|
|---|---|
| Molecular Weight |
360.2053
|
| CAS # |
153436-54-5
|
| Related CAS # |
PD153035 Hydrochloride;183322-45-4
|
| SMILES |
BrC1=C([H])C([H])=C([H])C(=C1[H])N([H])C1C2=C([H])C(=C(C([H])=C2N=C([H])N=1)OC([H])([H])[H])OC([H])([H])[H]
|
| Synonyms |
PD153035; PD 153035; PD-153035; ZM 252868; Tyrphostin AG 1517; AG 1517; ZM 252868;ZM-252868; ZM252868; SU-5271, SU 5271;SU5271;
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
|
|||
|---|---|---|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.94 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. Solubility in Formulation 2: 30% propylene glycol, 5% Tween 80, 65% D5W:30mg/mL (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
PD153035 reversesABCG2mediated drug resistance by blocking the function of ABCG2 transporter.Cancer Lett.2018 Jun 28;424:19-29. |
|---|
PD153035 increases the intracellular concentration of [3H]-MX in ABCG2 overexpressing cells.Cancer Lett.2018 Jun 28;424:19-29. |
PD153035 increases ABCG2 hydrolysis of ATP.Cancer Lett.2018 Jun 28;424:19-29. |
PD153035 decreases expression of ABCG2 on ABCG2 overexpressing cells.Cancer Lett.2018 Jun 28;424:19-29. |
|---|
The effect of PD153035 on the growth of ABCG2-expressing tumors in nude athymic mice.Cancer Lett.2018 Jun 28;424:19-29. |
Binding geometry of PD153035 into ABCG2 binding pocket by Glide docking algorithms.Cancer Lett.2018 Jun 28;424:19-29. |
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA
