(S)-crizotinib --- MTH1 Inhibitor
| Overview | |
| Catalog # | bs-60208C |
| Product Name | (S)-crizotinib --- MTH1 Inhibitor |
| Specifications | |
| Storage Buffer | Powder |
| Storage Condition | Powder: 4C for 1 year, -20C for 3 years. DMSO: 4C for 3 month. |
| Target | |
| Product Information | Molecular Weight: 450.34 Formula: C21 H22 Cl2 F N5 O CAS Number: 1374356-45-2 InChi Key: KTEIFNKAUNYNJU-LBPRGKRZSA-N InChi: InChI=1S/C21H22Cl2FN5O/c1-12(19-16(22)2-3-17(24)20(19)23)30-18-8-13(9-27-21(18)25)14-10-28-29(11-14)15-4-6-26-7-5-15/h2-3,8-12,15,26H,4-7H2,1H3,(H2,25,27)/t12-/m0/s1 Smiles: C[C@H](OC1=CC(=CN=C1N)C1=CN(N=C1)C1CCNCC1)C1C(Cl)=CC=C(F)C=1Cl Purity: 98.0 Solubility: DMSO: 42 mg/mL (93.26 mM); EtOH: 22 mg/mL (48.85 mM). Appearance: Solid powder Shelf Life: 3.0 years |
| Description | (S)-Crizotinib is a novel potent, selective and cell permeable MTH1 inhibitor with an IC50 of ~72 nM. MTH1 is a nucleotide pool sanitizing enzyme. (S)-Crizotinib disrupts nucleotide pool homeostasis via MTH1 inhibition and induces an increase in DNA single-strand breaks in cancer cells. In vivo it can effectively suppress tumor growth in colon carcinoma xenograft model by once per day oral dosing. (R)-Crizotinib, which is (R)-enantiomer of the drug, is inactive against MTH1 in vitro. Loss-of-function of MTH1 impaired growth of KRAS tumor cells. (S)-Crizotinib is a useful chemical probe to further validate MTH1 as a promising novel class of anticancer target. |
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