1. Cell Cycle/DNA Damage
    Apoptosis
  2. DNA/RNA Synthesis
    Apoptosis
  3. (S)-Crizotinib

(S)-Crizotinib 

Cat. No.: HY-100549
Handling Instructions

(S)-Crizotinib, a (S)-enantiomer of crizotinib, is a potent and selective MTH1 (mutT homologue) inhibitor with an IC50 of 330 nM. (S)-Crizotinib disrupts nucleotide pool homeostasis via MTH1 inhibition, induces an increase in DNA single strand breaks, activates DNA repair in human colon carcinoma cells, and effectively suppresses tumour growth in animal models.

For research use only. We do not sell to patients.

(S)-Crizotinib Chemical Structure

(S)-Crizotinib Chemical Structure

CAS No. : 1374356-45-2

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Description

(S)-Crizotinib, a (S)-enantiomer of crizotinib, is a potent and selective MTH1 (mutT homologue) inhibitor with an IC50 of 330 nM. (S)-Crizotinib disrupts nucleotide pool homeostasis via MTH1 inhibition, induces an increase in DNA single strand breaks, activates DNA repair in human colon carcinoma cells, and effectively suppresses tumour growth in animal models[1].

IC50 & Target

IC50: 330 nM (MTH1)[1]

In Vitro

(S)-crizotinib (0.625-80 μM; 24 hours) decreases the viability of NCI-H460, H1975 and A549 cells with IC50 values of 14.29, 16.54 and 11.25 μM, respectively[2].
(S)-crizotinib (10-30 μM; 24 hours) induces NCI-H460, H1975 and A549 cells apoptosis[2].
(S)-crizotinib (10-30 μM; 24 hours) decreases Bcl-2: Bax ratio. (S)-crizotinib decreases B cell lymphoma 2 (Bcl-2), and Bcl-2 associated protein x (Bax) is either unaltered (H460 cells) or shows an increase (H1975 cells)[2].
(S)-Crizotinib induces apoptosis in human non-small cell lung cancer (NSCLC) cells by activating ROS-dependent ER stress apoptotic pathway independent of mutT homologue (MTH1)[2].

Cell Viability Assay[2]

Cell Line: NSCLC cells, NCI-H460, H1975 and A549 cells
Concentration: 0.625, 1.25, 2.5, 5, 10, 20, 40, 60, 80 μM
Incubation Time: 24 hours
Result: Decreased the viability of NCI-H460, H1975 and A549 cells with IC50 values of 14.29, 16.54 and 11.25 μM, respectively.

Apoptosis Analysis[2]

Cell Line: NSCLC cells, NCI-H460, H1975 and A549 cells
Concentration: 10, 20 or 30 μM
Incubation Time: 24 hours
Result: Induced cells apoptosis.

Western Blot Analysis[2]

Cell Line: NSCLC cells, NCI-H460, H1975 and A549 cells
Concentration: 10, 20 or 30 μM
Incubation Time: 24 hours
Result: Decreased Bcl-2: Bax ratio.
In Vivo

(S)-crizotinib (7.5 or 15 mg/kg; intraperitoneal injections; once daily for 10 days) results in significant reductions in both tumor volume and tumor weight[2].

Animal Model: Five-week-old, athymic BALB/c nu/nu female mice (17-19 g) with NCI-H460 cells[2]
Dosage: 7.5 or 15 mg/kg
Administration: Intraperitoneal injections; once daily for 10 days
Result: Resulted in significant reductions in both tumor volume and tumor weight.
Molecular Weight

450.34

Formula

C₂₁H₂₂Cl₂FN₅O

CAS No.

1374356-45-2

SMILES

NC1=NC=C(C2=CN(C3CCNCC3)N=C2)C=C1O[[email protected]](C4=C(Cl)C=CC(F)=C4Cl)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility
In Vitro: 

DMSO : 12.5 mg/mL (27.76 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2205 mL 11.1027 mL 22.2054 mL
5 mM 0.4441 mL 2.2205 mL 4.4411 mL
10 mM 0.2221 mL 1.1103 mL 2.2205 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 1.25 mg/mL (2.78 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 1.25 mg/mL (2.78 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 1.25 mg/mL (2.78 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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(S)-Crizotinib
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