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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
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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

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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.
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.

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