PD153035 HCl 183322-45-4

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Molecular Weight:

396.67 PD153035 is a potent and specific inhibitor of EGFR with Ki and IC50 of 5.2 pM and 29 pM; little effect noted against PGDFR, FGFR, CSF-1, InsR and Src.


Biological Activity


PD 153035 shows a potent and selective inhibitory effect on tyrosine
phosphorylation induced with EGF with IC50 of 15 nM and 14 nM in Swiss
3T3 fibroblast and A-431 human epidermoid carcinoma cells, respectively. PD153035 shows growth inhibitory effects in cultures of
EGF receptor-overexpressing human cancer cell lines including A431,
Difi, DU145, MDA-MB-468 and ME180 cells with IC50 of 0.22 μM, 0.3μM, 0.4
μM, 0.68 μM and 0.95 μM, respectively.


PD153035 induces a
dose-dependent growth inhibition in nasopharyngeal carcinoma (NPC)
cells including NPC-TW01, NPC-TW04, and HONE1 cell lines with IC50 of
12.9 μM, 9.8 μM and 18.6μM, respectively. A recent study
shows that PD153035 abolishes COX-2 expression induced by the
PAR(2)-activating peptide 2-furoyl-LIGRLO-NH(2) (2fLI) in Caco-2 colon
cancer cells.


In A431 human epidermoid tumors grown as xenografts in immunodeficient
nude mice, PD153035 at 80 mg/kg inhibit EGF receptor tyrosine kinase
activity. PD153035 improves glucose tolerance, insulin sensitivity, and signaling and reduces subclinical inflammation in HFD-fed mice. Pretreatment of EGFR Inhibitors by 24 hours significantly enhances the
cytotoxic effect of doxorubicin, paclitaxel, cisplatin, and
5-fluororuacil in NPCTW04 cells.


Protocol(Only for Reference)


Kinase Assay: [1]

Inhibition of EGF receptor tyrosine kinase

Enzyme reactions are performed in a total volume of 0.1 mL containing 25 mM Hepes (pH 7.4), 5 mM MgCl2, 2 mM MnCl2, 50 μM sodium vanadate, 0.5 to 1.0 ng of enzyme (which also contains enough EGF to make the final concentrations 2 μg/mL), 10 μM ATP containing 1 μCi of [32P]ATP, varying concentrations of PD153035, and 200 μM of a substrate peptide based on a portion of phospholipase C-γl having the sequence Lys-His-Lys-Lys-Leu-Ala-Glu-Gly-Ser-Ala-Tyr472-Glu-Glu-Val. The reaction is initiated by the addition of ATP. After 10 minutes at room temperature, the reaction is terminated by addition of 2 mL of 75 mM phosphoric acid, and the solution is passed through a 2.5-cm phosphocellulose filter disk that binds the peptide. The filter is washed five times with 75 mM phosphoric acid and placed in a vial with 5 mL of scintillation fluid. The uninhibited control activity produces approximately 100,000 cpm.

Cell Assay: [2]

Cell lines	A431, Difi, DU145, MDA-MB-468 and ME180
Concentrations	0-3 μM
Incubation Time	72 hours
Method	Cells are seeded in sixwell plates. The next day, cells are changed to medium containing 0.5% FBS for 18 hours, and then PD153035 is added at various concentrations to the cultures. After 72 hours of treatment, cells are washed once with PBS, harvested with 0.1% human trypsin-l mM EDTA in PBS, and counted with a Coulter counter. The CMK cells grow in suspension and, therefore, do not require trypsinization.

Animal Study: [5]

Animal Models	A431 cells are injected into the outbred nude mice.
Formulation	PD153035 is dissolved in water.
Dosages	≤80 mg/kg
Administration	Administered via i.p.
Solubility	30% propylene glycol, 5% Tween 80, 65% D5W, 30 mg/mL
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

Species	Baboon	Dog	Monkey	Rabbit	Guinea pig	Rat	Hamster	Mouse
Weight (kg)	12	10	3	1.8	0.4	0.15	0.08	0.02
Body Surface Area (m2)	0.6	0.5	0.24	0.15	0.05	0.025	0.02	0.007
Km factor	20	20	12	12	8	6	5	3

Animal A (mg/kg) = Animal B (mg/kg) multiplied by	Animal B Km
	Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×	mouse Km(3)	= 11.2 mg/kg
	rat Km(6)

Chemical Information

Molecular Weight (MW)	396.67
Formula	C16H14BrN3O2.HCl
CAS No.	183322-45-4

Storage	3 years -20℃Powder
	6 months-80℃in solvent (DMSO, water, etc.)
Synonyms	SU-5271 (AG1517) HCl ,ZM 252868 HCl

Solubility (25°C) *	In vitro	DMSO	0.5 mg/mL (1.26 mM)
		Water	<1 mg/mL (
		Ethanol	<1 mg/mL (
	In vivo	30% propylene glycol, 5% Tween 80, 65% D5W	30 mg/mL
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Name	N-(3-bromophenyl)-6,7-dimethoxyquinazolin-4-amine hydrochloride

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