XL413 (hydrochloride) Chemical Properties

storage temp. 

Store at -20°C

solubility 

DMSO:0.2(Max Conc. mg/mL);0.613(Max Conc. mM)
PBS (pH:7.2):10.0(Max Conc. mg/mL);30.66(Max Conc. mM)

form 

A crystalline solid

color 

White to off-white

XL413 (hydrochloride) Usage And Synthesis

Description

XL413 is a potent inhibitor of Cdc7 (IC₅₀ = 3.4 nM). It is >60, >10, and >300-fold selective for Cdc7 over CK2, PIM1, and a panel of over 100 protein kinases, respectively. XL413 inhibits the growth of MDA-MB-231T and COLO 205 cells (IC₅₀s = 118 and 140 nM, respectively). It inhibits Cdc7-specific phosphorylation of mini-chromosome maintenance protein (MCM2) and induces cell cycle accumulation in the S and G₂ phases in MDA-MB-231T and COLO 205 cells that overexpress Cdc7. In vivo, XL413 inhibits MCM2 phosphorylation (ED₅₀ = <3 mg/kg) and reduces tumor growth in a COLO 205 mouse xenograft model when administered orally at doses of 10, 30, and 100 mg/kg.

Uses

XL413 (BMS-863233) hydrochloride is a potent, selective and ATP competitive inhibitor of Cdc7, with an IC50 of 3.4 nM, and also shows potent effect with IC50s of 215, 42 nM on CK2, PIM1, respectively, and an EC50 of 118 nM on pMCM.

in vivo

IC 50

Cdc7: 3.4 nM (IC₅₀); PIM1: 42 nM (IC₅₀); CK2: 215 nM (IC₅₀)

References

[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. DOI:10.1016/j.bmcl.2012.04.024
[2] Sasi NK, et al. The potent Cdc7-Dbf4 (DDK) kinase inhibitor XL413 has limited activity in many cancer cell lines and discovery of potential new DDK inhibitor scaffolds. PLoS One. 2014 Nov 20;9(11):e113300. DOI:10.1371/journal.pone.0113300

XL413 (hydrochloride)(2062200-97-7)Related Product Information

• XL 228
• XL-019
• 3-Acridinecarboxamide, 9-chloro-5,6,7,8-tetrahydro-N-[(4S)-5-[4-hydroxy-4-[[7-[[3-(4-methyl-1-piperazinyl)-1-oxopropyl]amino]-4-oxo-3(4H)-quinazolinyl]methyl]-1-piperidinyl]-5-oxo-4-(phenylmethyl)pentyl]-
• XL-388
• BMS-908662
• XL888
• XL765
• 2-methoxyethyl 4-((4-(4-chlorophenoxy)-3,5-difluorophenyl)sulfonyl)-3-(hydroxycarbamoyl)piperazine-1-carboxylate