WZ8040 1214265-57-2

.cp_wz table {border-top: 1px solid #ccc;border-left:1px solid #ccc; } .cp_wz table td{border-right: 1px solid #ccc; border-bottom: 1px solid #ccc; padding: 5px 0px 0px 5px;} .cp_wz table th {border-right: 1px solid #ccc;border-bottom: 1px solid #ccc; padding: 5px 0px 0px 5px;}


Molecular Weight:

481.01 WZ8040 is a novel mutant-selective irreversible EGFRT790M inhibitor, does not inhibit ERBB2 phosphorylation (T798I).


Biological Activity


WZ8040 is 30- to 100-fold more potent against EGFR T790M, and up to
100-fold less potent against wild-type EGFR, than quinazoline-based EGFR
Inhibitors such as CL-387785 and HKI-272. WZ8040 treatment potently
inhibits the growth of HCC827 (EGFR Del E746_A750), PC9 (EGFR Del
E746_A750), H3255 (EGFR L858R), H1975 (EGFR L858R/T790M), and PC9 GR
(EGFR Del E746_A750/T790M) with IC50 of 1 nM, 6 nM, 66 nM, 9 nM, and 8
nM, respectively.


WZ8040 weakly inhibits the growth of HCC827 GR (EGFR
E746_A750/MET amp), H1819 (ERBB2 amp), Calu-3 (ERBB2 amp), H1781 (ERBB2
Ins G776V, C), and HN11 (EGFR & ERBB2 WT) with IC50 of >3.3 μM,
738 nM, 915 nM, 744 nM, and 1.82 μM, respectively. WZ8040 is not toxic
up to 10 μM against A549 (KRAS mutant) or H3122 (EML4-ALK) cells.


Protocol(Only for Reference)


Cell Assay: [1]

Cell lines	HCC827, H3255, HCC827 GR, H1975, PC9, PC9 GR, Calu-3, H1819, and Ba/F3
Concentrations	Dissolved in DMSO, final concentrations ~10 μM
Incubation Time	72 hours
Method	Cells are exposed to increasing concentrations of WZ8040 for 72 hours. Growth is assessed using the MTS survival assay.

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)	481.01
Formula	C24H25ClN6OS
CAS No.	1214265-57-2

Storage	3 years -20℃Powder
	6 months-80℃in solvent (DMSO, water, etc.)
Synonyms

Solubility (25°C) *	In vitro	DMSO	96 mg/mL (199.58 mM)
		Water	<1 mg/mL (
		Ethanol	3 mg/mL (6.23 mM)
* <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-(5-chloro-2-(4-(4-methylpiperazin-1-yl)phenylamino)pyrimidin-4-ylthio)phenyl)acrylamide

Molarity Calculator
Dilution Calculator
Molecular Weight Calculator

Contact us if you need more details on 1214265-57-2. We are ready to answer your questions on packaging, logistics, certification or any other aspects about WZ8040 1214265-57-2、1214265-57-2 WZ8040. If these products fail to match your need, please contact us and we would like to provide relevant information.

Product Categories : Protein Tyrosine Kinase > EGFR Inhibitor