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SGX523

Item № 18093
CAS № 1022150-57-7
Purity ≥98%
product image
                (CAS 1022150-57-7)
SIZE PRICE QUANTITY SUBTOTAL
CART TOTAL
     1 mg $35.00 0.00
     5 mg $131.00 0.00
     10 mg $228.00 0.00
     25 mg $438.00 0.00

Pricing updated 2019-04-24. Prices are subject to change without notice.

Description

The hepatocyte growth factor receptor c-Met commonly shows elevated activity in several forms of cancer.1,2 SGX523 is a potent, selective, ATP-competitive inhibitor that blocks the tyrosine kinase activity of c-Met with an IC50 value of 4 nM.1 It is over 1,000-fold selective for c-Met over a panel of other kinases.1 SGX523 is orally active and dose-dependently inhibits the growth of a variety of tumor xenografts in mice.1,3 The effectiveness of SGX523 is enhanced when combined with other chemotherapeutic compounds, including inhibitors of EGFR.2,4 SGX523 is metabolized, at least in part, by aldehyde oxidase, an enzyme that differs in activity across different species.5

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Technical Information
Formal Name
6-[[6-(1-methyl-1H-pyrazol-4-yl)-1,2,4-triazolo[4,3-b]pyridazin-3-yl]thio]-quinoline
CAS Number
1022150-57-7
Molecular Formula
C18H13N7S
Formula Weight
359.4
Purity
≥98%
Formulation
A crystalline solid
λmax
212, 234 nm
SMILES
CN1N=CC(C2=NN3C(SC4=CC5=CC=CN=C5C=C4)=NN=C3C=C2)=C1
InChI Code
InChI=1S/C18H13N7S/c1-24-11-13(10-20-24)16-6-7-17-21-22-18(25(17)23-16)26-14-4-5-15-12(9-14)3-2-8-19-15/h2-11H,1H3
InChI Key
BCZUAADEACICHN-UHFFFAOYSA-N

Warning - this product is not for human or veterinary use.

Shipping & Storage
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
Stability
≥ 2 years
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Additional Information

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References & Product Citations
Product Description References

1. Buchanan, S.G., Hendle, J., Lee, P.S., et al. SGX523 is an exquisitely selective, ATP-competitive inhibitor of the MET receptor tyrosine kinase with antitumor activity in vivo Molecular Cancer Therapeutics 8(12), 3181-3190 (2009).

2. Padda, S., Neal, J.W., and Wakelee, H.A. MET inhibitors in combination with other therapies in non-small cell lung cancer Transl.Lung Cancer Res. 1(4), 238-253 (2012).

3. Guessous, F., Zhang, Y., diPierro, C., et al. An orally bioavailable c-Met kinase inhibitor potently inhibits brain tumor malignancy and growth Anticancer Agents Med.Chem. 10(1), 28-35 (2010).

4. Zhang, Y.W., Staal, B., Essenburg, C., et al. Strengthening context-dependent anticancer effects on non-small cell lung carcinoma by inhibition of both MET and EGFR Molecular Cancer Therapeutics 12(8), 1429-1441 (2013).

5. Diamond, S., Boer, J., Maduskuie, T.P., Jr., et al. Species-specific metabolism of SGX523 by aldehyde oxidase and the toxicological implications Drug Metabolism and Disposition 38(8), 1277-1285 (2010).

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