(S)-crizotinib

SKU: orb1300839

Description

(S)-Crizotinib (ent-crizotinib) is the (S)-enantiomer of crizotinib and acts as a potent MTH1 inhibitor with an IC50 of 72 nM. This small molecule is a valuable research tool for studying the role of MTH1 in DNA repair mechanisms, applicable in both in vitro and in vivo cancer research contexts.

Research Area

Cell Biology, Molecular Biology

Key Properties

• CAS Number: 1374356-45-2
• MW: 450.34
• Purity: 99.89% (May vary between batches)
• Formula: C₂₁H₂₂Cl₂FN₅O
• SMILES: C[C@H](Oc1cc(cnc1N)-c1cnn(c1)C1CCNCC1)c1c(Cl)ccc(F)c1Cl
• Target: Apoptosis,MTH1,DNA/RNA Synthesis
• Solubility: 1eq. HCl:9 mg/mL (19.98 mM);DMSO:22.5 mg/mL (49.96 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (2.22 mM)

Bioactivity

• Target IC50:
  MTH1:72 nM
• In Vivo:
  (S)-crizotinib activates DNA repair mechanisms in human colorectal cancer cells by inhibiting MTH1, thereby disrupting nucleotide pool homeostasis and further inducing an increase in DNA single-strand breaks.
• In Vitro:
  In the SW480 colorectal cancer model, daily oral administration of 50mg/kg (S)-Crizotinib effectively inhibits tumor growth.
• Cell Research:
  One day before treatment, cells are seeded per well in six-well plates and incubated for 24 h. The next day DMSO (equal to highest amount of compound dilution, maximum 0.2%) or compounds in increasing concentrations were added and cells incubated at 37 °C, 5% CO2, for 7-10 days. After washing with PBS, cells are fixed with ice-cold methanol, stained with crystal violet solution (0.5% in 25% methanol) and left to dry overnight. For quantification of results, ultraviolet absorbance of crystal violet is determined at 595 nm following solubilisation by 70% ethanol. Data are analysed using nonlinear regression analysis using the GraphPad Prism software. (Only for Reference)

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

DNASynthesis, DNA/RNA Synthesis, DNA Synthesis, crizotinib, anticancer, Apoptosis, (S) crizotinib, (S)crizotinib, (S)-Crizotinib, activity, mutT, inhibit, MTH1, nucleotide, homologue, Inhibitor, ent-crizotinib, RNA Synthesis, RNASynthesis, pool

Compound Identifiers

PubChem CID

56671814