(S)-crizotinib, MTH1 Inhibitor


Catalog No. size PriceQuantity
M60208-2S 2 mg solid $99
M60208-10S 10mg solid $396

Description

Product Information
Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.
Solubility: DMSO up to 50 mM
Chemical Name: (S)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1-(piperidin-4-yl)-1H-pyrazol-4-yl)pyridin-2-amine
Purity: ≥98%
CAS#: 1374356-45-2
Molecular Weight: 450.34
Formula: C21H22Cl2FN5O


Biological Activity:

(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.

How to Use:

In vitro: (S)-Crizotinib was used at 2-10 µM final concentration in various in vitro and cellular assays.

In vivo:(S)-Crizotinib was dosed to mice orally at 50?mg/kg once per day to impair tumor growth in an SW480 colon carcinoma xenograft model. Formulation is 1% DMSO, 10% ethanol, 10% Cremophor, 10% Tween 80, 69% PBS.

Reference:

  • 1. Huber KV, et al. Stereospecific targeting of MTH1 by (S)-crizotinib as an anticancer strategy. (2014) Nature. 508(7495):222-7.



Products are for research use only. Not for human use.


Payment & Security

American Express Apple Pay Diners Club Discover Elo Google Pay JCB Mastercard PayPal Shop Pay Venmo Visa

Your payment information is processed securely. We do not store credit card details nor have access to your credit card information.

Estimate shipping

You may also like

Recently viewed