Tel: 732-484-9848
Fax: 888-484-5008
Email: [email protected]
   
Building blocks
Intermediates
Bioactive molecules
Product Pathways
All Targets
Anti-infection
Antibody-drug conjugate....
Apoptosis
Autophagy
Biochemical Reagent
Cell Cycle/DNA Damage
Cytoskeleton
Epigenetics
GPCR/G protein
Immunology/Inflammation
JAK/STAT Signaling
MAPK/ERK Pathway
Membrane Transporter/Io....
Metabolic Enzyme/Protease
Neuronal Signaling
NF-κB
Others
PI3K/Akt/mTOR
Protein Tyrosine Kinase....
Stem Cells/Wnt
TGF-beta/Smad
Vitamin D Related
Research Area
Cancer
Cardiovascular Disease
Endocrinology
Infection
Metabolic Disease
Neurological Disease
Others
Inflammation/Immunology
Product Type
All Products
New Products
Featured Products
Home   »   Product Pathways  »    »  XL413

Products are for research use only. Not for human use. We do not sell to patients.


CS-1956 XL413


(XL-413;XL 413)
Structure Price and Availability of    XL413
United States
Size Price Stock
5mg $143 Backordered Inquiry Please send us inquire for the availability about
CS-1956
10mg $200 Backordered
50mg $600 Backordered
100mg $900 Backordered
200 mg Get quote
500 mg Get quote
 Distributor In Japan:  フナコシ株式会社 www.funakoshi.co.jp    電話番号:81-3-5684-1620   
 FAX番号:81-3-5684-1775
Inquiry for price and availability only. Please place your order via our email or fax.
Contact us for competitive discounts on bulk quantities .
  • Data Sheet
  • Introduction
  • References
  • Related Products

XL413  M.Wt:  289.72
XL413  Formula: C14H12ClN3O2
XL413  Solubility: 10 mM in DMSO
XL413  Purity: >98%
XL413  Storage:  Please store the product under the recommended conditions in the Certificate of Analysis.
CAS: 1169558-38-6

View current batch:

XL413 is a potent and selective Cdc7 inhibitor with an IC50 of 3.7 nM, >60-fold selectivity against CK2, >10-fold selectivity against PIM, and >300-fold selectivity against a panel of over 100 protein kinases. IC50 value: 3.7 nM [1] Target: Selective Cdc 7 XL413 demonstrated excellent plasma exposures in mice [100 mg/kg (PO): 141 lM (1 h), 81 lM (4 h)]. Prolonged treatment with XL413 (3 days) inhibited the cell proliferation (IC50 = 2685 nM), decreased cell viability (IC50 = 2142 nM) and elicited the caspase 3/7 activity (EC50 = 2288 nM) in Colo-205 cells.XL413 demonstrated an excellent exposure profile in full rat PK assay (dosed at 3 mg/kg: Cmax (PO) = 8.61 lM, AUC (po) = 75 lM h, CL = 117 mL/h kg, Vss = 0.55 L/kg, T1/2 = 2.32 h, F = 95%). Tumor bearing mice were administered XL413 orally at doses of 10, 30, or 100 mg/kg once daily (qd) for 14 days,XL413 was well tolerated at all the doses and regimens examined, with no significant body weight loss observed [1].

[1]. Koltun ES, et al. Discovery of XL413, a potent and selective CDC7 inhibitor. Bioorg Med Chem Lett. 2012 Jun 1;22(11):3727-31.
Abstract
CDC7 is a serine/threonine kinase that has been shown to be required for the initiation and maintenance of DNA replication. Up-regulation of CDC7 is detected in multiple tumor cell lines, with inhibition of CDC7 resulting in cell cycle arrest. In this paper, we disclose the discovery of a potent and selective CDC7 inhibitor, XL413 (14), which was advanced into Phase 1 clinical trials. Starting from advanced lead 3, described in a preceding communication, we optimized the CDC7 potency and selectivity to demonstrate in vitro CDC7 dependent cell cycle arrest and in vivo tumor growth inhibition in a Colo-205 xenograft model.

Keywords: buy XL413 | XL413 Supplier | purchase XL413 | XL413 cost | XL413 manufacturer | order XL413 | XL413 distributor | XL413 structure,chemscene
buy 1169558-38-6 | 1169558-38-6 Supplier | purchase 1169558-38-6 | 1169558-38-6 cost | 1169558-38-6 manufacturer | order 1169558-38-6 | 1169558-38-6 distributor | 1169558-38-6 structure,chemscene


CHEMSCENE, LLC
Tel: 732-484-9848
Fax: 888-484-5008
Email:  [email protected]
Address: 11 Deer Park Drive, Suite 102D Monmouth Junction, NJ 08852.
Products are for research use only. Not for human use. We do not sell to patients. Sitemap | Inhibitor © Copyright 2012. All Rights Reserved.