Varlitinib Inhibitor CAS No. 845272-21-1

Cat. No.	Name	Size	Price
KI1499	Varlitinib	5 mg	$432
	Varlitinib	10 mg	$592
	Varlitinib	50 mg	$1712
	Varlitinib	200 mg	$3952

Chemical Characteristic

Product Name	Varlitinib
Synonyms	ARRY-334543
CAS No.	845272-21-1
Molecular Weight	466.94
Formula	C₂₂H₁₉ClN₆O₂S
Chemical Name	4-N-[3-chloro-4-(1,3-thiazol-2-ylmethoxy)phenyl]-6-N-[(4R)-4-methyl-4,5-dihydro-1,3-oxazol-2-yl]quinazoline-4,6-diamine
Smiles	n1cnc(c2cc(ccc12)NC1=N[C@@H](CO1)C)Nc1cc(c(cc1)OCc1sccn1)Cl
Chemical Structure
Documents	LCMS

Biological activities

Varlitinib is a reversible, ATP-competitive inhibitor with nanomolar potency in both in vitro and in cell-based assays showing strong activity against EGFR, ErbB2 and ErbB4. The IC50 of varlitinib is 7, 0.5 and 4 nM against EGFR, ErbB2 and ErbB4, respectively. Varlitinib inhibits A431 and BT474 cells carrying EGFR, ErbB2 and ErbB4 with IC50 of 43, 36 and 130 nM, respectively.^[1] Varlitinib is assembled convergently from a thiourea core and an aniline head group. In the A431 (EGFR-overexpressor) human epidermoid carcinoma xenograft model, dose-dependent inhibition of tumor growth by varlitinib is observed. Varlitinib at the doses of 50 mg/kg, BID results in greater than 50% tumor growth inhibition. In the Calu-3 xenograft model, significant tumor growth inhibition is observed at 100 mg/kg, BID with 8/8 animals showing regression of their tumors by varlitinib. Varlitinib has broad anti-tumor effects in vivo in EGFR wide type and mutant cells in xenograft models, as well as in ErbB-2 driven tumor models.^[2]

References

[1] Wallance Eli, et al. Selective Inhibitors of the ErbB-Family of Receptor Tyrosine Kinase. 2011. [2] Pheneger Tracy, et al. In Vivo Anti-Tumor Activity of ARRY-334543, a Small Molecule Inhibitor of EGFR and ErbB-1. Abstracts.

Please click here to fill online order form, and we will make sure to supply you product with detail information. This process usually takes between 24 to 48 hours, depending on products stock avaliability. All inquires and subsequent projects are handled in the strictest confidence and will be backed by a confidentiality agreement if required.

KareBay^TM provides scientists and clinicians with a wide range of biotechnological products and science lab supplies for chemical research and analyzing life processes. KareBay's extensive capabilities include commercializing reagents and kits, manufacturing biotech products and providing contract research services to organizations worldwide. Our many global labs, offices, and business partners enable KareBay to extend its products and services to its customer base around the world.

Our products are used for research, laboratory and further evaluation purposes. They are not for human use.

About

KareBay^TM Biochem
Sitemap
Blog

Custom Services