XL413 hydrochloride

SKU: orb1300515

Description

XL413 hydrochloride is a potent, selective, and ATP-competitive inhibitor of Cdc7 kinase (IC50 = 3.4 nM). It also inhibits CK2 and PIM1 and has been utilized in preclinical research to study DNA replication and cell cycle progression in various cancer models, both in vitro and in vivo.

Research Area

Cell Biology, Epigenetics & Chromatin, Metabolism Research, Pharmacology & Drug Discovery, Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 2062200-97-7
• MW: 326.18
• Purity: 99.82%
• Formula: C₁₄H₁₃Cl₂N₃O₂
• SMILES: Cl.Clc1ccc2oc3c(nc([nH]c3=O)[C@@H]3CCCN3)c2c1
• Target: CDK,Casein Kinase,Pim,Cholecystokinin Receptor
• Solubility: DMSO:2.5 mg/mL (7.66 mM);H2O:4.76 mg/mL (14.59 mM)

Bioactivity

• Target IC50:
  CDC7:3.4 nM|Pim1:42 nM|CK2:212 nM
• In Vivo:
  XL413 (BMS-863233; 100 mg/kg, p.o.) hydrochloride shows excellent plasma exposure and favorable pharmacokinetic properties in mice. Additionally, XL413 hydrochloride (10, 30, or 100 mg/kg, p.o.) is well tolerated at all tested doses without significant body weight loss .
• In Vitro:
  XL413 (BMS-863233) hydrochloride effectively inhibits cell proliferation (IC 50 = 2685 nM), reduces cell viability (IC 50 = 2142 nM), and increases caspase 3/7 activity (EC 50 = 2288 nM) in Colo-205 cells. Additionally, it significantly suppresses the anchorage-independent growth of Colo-205 cells in soft agar (IC 50 = 715 nM) . Demonstrating cytotoxic effects, XL413 hydrochloride has IC 50 values of 22.9 μM in HCC1954 cells and 1.1 μM in Colo-205 cells. It triggers apoptosis in Colo-205 cells without affecting HCC1954 cells. As a DDK inhibitor, XL413 shows potent activity in vitro (IC 50 = 22.7 nM), yet fails to inhibit DDK-dependent Mcm2 phosphorylation in HCC1954 cells, while remaining effective in Colo-205 cells .

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

BMS 863233, BMS 863233 Hydrochloride, BMS863233, BMS863233 Hydrochloride, BMS-863233 Hydrochloride, Casein Kinase, CaseinKinase, Cdc7, CK2, XL 413 Hydrochloride, XL 413, XL-413, Pim1

Compound Identifiers

PubChem CID

135564631