(S)-crizotinib

Research use only, not for human use.

(S)-crizotinib（IC50 of 72 nM）, an effective MTH1 (NUDT1) inhibitor, is the (S)-enantiomer of crizotinib.

(S)-Crizotinib is an MTH1 inhibitor. By inhibiting MTH1, (S)-Crizotinib disrupts nucleotide pool homeostasis, induces an increase in DNA single-strand breaks, activates DNA repair in human colon carcinoma cells, and effectively suppresses tumor growth in animal models.

Cell Viability Assay 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 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 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.

Animal Model:Five-week-old, athymic BALB/c nu/nu female mice (17-19 g) with NCI-H460 cells 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.

(S)-Crizotinib | S-Crizotinib

GPCR/G Protein

Calcium Channel

MTH1

Cancer

——

1374356-45-2

450.34

C21H22Cl2FN5O

>98% (HPLC)

In Vitro:?DMSO : 12.5 mg/mL (27.76 mM)

C[C@@H](c1c(ccc(c1Cl)F)Cl)Oc1c(ncc(c1)c1cn(nc1)C1CCNCC1)N

3-[(1S)-1-(2,6-Dichloro-3-fluorophenyl)ethoxy]-5-[1-(4-piperidinyl)-1H-pyrazol-4-yl]-2-pyridinamine

(-20℃)

With Ice Pack

≥ 2 years