PD153035 HCl Chemical Structure
BIBW2992 (Afatinib, Tomtovok, Tovok) irreversibly inhibits EGFR/HER2 including EGFRwt, EGFR L858R , EGFR L858R/T790M and HER2 with IC50 of 0.5 nM, 0.4 nM, 10 nM, 14 nM, respectively.
CI-1033 is a potent tyrosine kinase inhibitor of EGFR and erbB2 with IC50 of 1.5 nM and 9.0 nM, respectively.
Erlotinib HCl also known as Tarceva, CP-358774, OSI-774, NSC-718781 is a HCL salt with IC50 of 2 nM for HER1/EGFR TK.
Gefitinib (Iressa) also known as ZD-1839 & Iressa is a novel potent EGFR tyrosine kinase & Akt phosphorylations inhibitor with IC50 of 37, 26 and 57 nM.
Lapatinib Ditosylate (Tyverb, GW-572016, GW-2016) is a potent purified EGFR and ErbB-2 inhibitor with IC50 of 10.2 and 9.8 nM, respectively.
Vandetanib (Zactima) is a VEGFR and EGFR antagonist and a tyrosine kinase inhibitor with IC50 of 60, 90, 40 nM for HUVEC proliferation, PC-9 cells and tyrosine kinase activity, respectively.
BMS-599626 (AC480) is a highly selective pan-HERKinase inhibitor with IC50 of 20 and 30 nM for the inhibition of HER1and HER2, respectively.
Inhibitor of the EGFR and ErbB2 with IC50 0.3 and 16 nM respectively.
AG 490 is a potent epidermal growth factor receptor kinase autophosphorylation inhibitor with an IC50 of 100 nM and 56.8 μM for EGFR and JAK, respectively.
WZ3146 is an irreversiblely inhibitor against EGFR T790M.
PD153035 hydrochloride is a hydrochloride acid salt form of PD153035 which is a ATP-competitive EGFR inhibitor with an IC50 and Ki of 25 and 6 pM.PD153035 effectively blocks the enhancement of mitogenesis, induction of early gene expression, and oncogenic transformation that occur in response to EGF receptor stimulation. With human fibroblasts and epidermoid carcinoma cells, PD153035 at nanomolar concentrations rapidly inhibits EGFR autophosphorylation. With breast and ovarian cancer cells, PD153035 not only blocks cell growth via inhibition of EGFR, but also upregulates the expression of the tumor suppressor retinoic acid receptor-beta 2 (RAR-beta2). [1][2]
| Molecular Weight (WM): | 396.67 |
|---|---|
| Formula: | C16H14BrN3O2.HCl |
| CAS No.: | 183322-45-4 |
| Synonyms: |
N/A
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| Dissolve in (25°C): | DMSO <1mg/mL |
| Water <1mg/mL | |
| Ethanol <1mg/mL | |
| Storage: | 2 years-20°CPowder |
| 1 week-4°Cin DMSO | |
| 1 month-80°in DMSO |
A collection of 864 bioactive compounds
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T47D cells were pretreated with 100ng/ml EGF for 15 min and then treated with the indicated concentrations of PD153035 for 24 hours.
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T47D cells were pretreated with 100ng/ml EGF for 15 min and then treated with the indicated concentrations of PD153035 for 24 hours.
Data independently produced by Dr. Zhang of Tianjin Medical University PD153035 HCl purchased from Selleck
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