ICONHome   ICONContact us   ICONAdd Favorites
Biochemtek
Search Product
Live Chat E-mail
Pharmacology
ICON Inhibitors
ICON Receptors
ICON Hedgehog Signaling Pathway
ICON Stem Cells & Wnt
ICON Signal Transduction
   More +
Research Area
ICON Cancer
ICON Antivirus
ICON Cardiovascular System
ICON Endocrinology
ICON Neuroscience
   More +
Product Type
ICON Natural Products
ICON Peptides
ICON Prostaglandins
ICON Vitamin D series compounds
ICON Toxins
   More +
Browse Alphabetically by Name
ALL A B C D E F
G H I J K L M
N O P Q R S T
U V W X Y Z Others
 
ICONC13463 CHIR-258(Dovitinib,TKI258) (405169-16-6)
 
 
Catalog No.: C13463
CAS No.: 405169-16-6
Synonym: TKI258,Dovitinib,Unii-I35H55G906
Chemical Name:

4-Amino-5-fluoro-3-[5-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]quinolin-2(1H)-one

Molecular Formula:

C21H21FN6O

Molecular Weight: 392.43
 
Technical Data:
Appearance:
Solubility: Soluble in DMSO
Purity: >99%
Storage: at -20℃ 2 years
Original QC Data:
Shipping Conditions: Ambient Temp.
 
Price and Availability of CHIR-258(Dovitinib,TKI258):

Size

Price

Stock

10mg 

USD

In stock 

50mg 

USD

In stock 

100mg 

USD

In stock 

Contact us for competitive discounts on bulk quantities

 
Biological Activity:
A multitargeted growth factor receptor kinase inhibitor to VEGFR, FGFR3, PDGFR and c-KIT. CHIR-258 was highly potent against FLT3 (1 nmol/L) with nanomolar activity against c-KIT (2 nmol/L), VEGFR1/2/3 (10 nmol/L); FGFR1/3 (8 nmol/L); PDGFRß (27 nmol/L) and CSF-1R (36 nmol/L). To confirm selectivity against class III, IV, and V RTKs, CHIR-258 was tested against other kinases in the phosphatidylinositol 3-kinase/Akt and mitogen-activated protein kinase pathways and was found to have negligible activity (IC50 > 10 Amol/L). CHIR-258 potently inhibited proliferation of MV4;11 cells in a dose-dependent manner with EC50 = 13 nmol/L. Although similar concentrationdependent effects on proliferation were observed with RS4; 11 cells, they were f24-fold less sensitive to CHIR-258 (EC50 =315 nmol/L). The antiproliferative effect of CHIR-258 was also tested on the FLT3 ITD mutant cells, MOLM13 and MOLM14 with EC50 concentrations similar to those seen with MV4;11 (EC50,6 nmol/L; data not shown). These data suggest that CHIR-258 is active on both FLT3 ITD and WT leukemic cells, with the constitutively active receptor being more sensitive to inhibition.
 
References:
1.Trudel S, et al. CHIR-258, a novel, multitargeted tyrosine kinase inhibitor for the potential treatment of t(4;14) multiple myeloma. Blood. 2005, 105(7), 2941-2948.
2. Huynh H, et al. Dovitinib demonstrates antitumor and antimetastatic activities in xenograft models of hepatocellular carcinoma. J Hepatol. 2012, 56(3), 595-601.
 
View Related Products by Target:
Nilotinib(AMN 107)
NVP-TAE684-TAE 684
Motesanib(AMG706)
Imatinib mesylate(STI-571)
BIBW 2992(Afatinib)
Dovitinib lactate(TKI258)
Pelitinib(EKB-569)
PF 2341066(Crizotinib)
ABT-869(Linifanib)
BIBF1120(Vargatef)
Brivanib alaninate(BMS-582664)
Lapatinib Ditosylate (GW-572016)
 
 

Keywords: Buy CHIR-258(Dovitinib,TKI258) | CHIR-258(Dovitinib,TKI258) Supplier | Purchase CHIR-258(Dovitinib,TKI258) | CHIR-258(Dovitinib,TKI258) Cost | CHIR-258(Dovitinib,TKI258)  Manufacturer | Order CHIR-258(Dovitinib,TKI258) | CHIR-258(Dovitinib,TKI258) Distributor | CHIR-258(Dovitinib,TKI258) Structure, Chembest

Buy 405169-16-6| 405169-16-6 Supplier | Purchase 405169-16-6 | 405169-16-6 Cost | 405169-16-6 Manufacturer | Order 405169-16-6 | 405169-16-6 Distributor | 405169-16-6 Structure, Chembest  

Products are for research use only. Not for human use. We do not sell to patients.
Copyright © 2010-2013 Chembest Research Laboratories. All Rights Reserved
E-mail:sales@biochembest.com