Language:English
Language:

Xcessbio

Place your promotion here

You have no items in your shopping cart.

(S)-crizotinib, MTH1 Inhibitor

Related Products

(S)-crizotinib, MTH1 Inhibitor

$99.00
A novel potent, selective and cell permeable MTH1 inhibitor.
Catalog No. Unit Price Qty
M60208-2s 2 mg soid $99.00

Details

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.

    S-Crizotinib_spec.pdf

    S-Crizotinib_MSDS.pdf



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


Description

Details

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.

    S-Crizotinib_spec.pdf

    S-Crizotinib_MSDS.pdf



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


Reviews

Write Your Review

How do you rate this product? *

Price:
Value:
Quality: