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Product Details

SHP099 | SHP2 inhibitor

SHP099 (1801747-11-4) is a potent (IC50 = 71 nM) and selective allosteric inhibitor of SHP2.  SHP2 is a non-receptor tyrosine phosphatase that regulates cell survival and proliferation through activating the RAS-ERK pathway. It also mediates programmed cell death 1 (PD-1) and T-lymphocyte attenuator (BTLA) immune checkpoint pathways.  Treatment with SHP099, incombination with ceritinib, halts growth of ALK-inhibitor resistant non-small-cell lung cancer cells.3  Thus, reduction of SHP2 activity is a potential important cancer therapy target.  It showed no activity against a panel of 21 other human phosphatases and 66 kinases.

References/Citations

1) Fortanet et al. (2016), Allosteric Inhibition of SHP2: Identification of a Potent, Selective, and Orally Efficacious Phosphatase Inhibitor; J. Med. Chem., 59 7773
2) Chen et al. (2016), Allosteric inhibition of SHP2 phosphatase inhibits cancers driven by receptor tyrosine kinases; Nature, 535 148
3) Dardaei et al. (2018), SHP2 inhibition restores sensitivity in ALK-rearranged non-small-cell lung cancer resistant to ALK inhibitors; Nat. Med. 24 512

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Catalog#  10-4604-0005

$70.00
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Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee.
 
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CAS:
180747-11-4
Catalog Number:
10-4604
Activity:
SHP2 inhibitor
Chemical Name:
6-(4-Amino-4-methylpiperidin-1-yl)-3-(2,3-dichlorophenyl)pyrazin-2-amine dihydrochloride
Molecular Weight:
425.18
Molecular Formula:
C16H19Cl2N5 • 2HCl
Solubility:
Soluble in DMSO (up to 5 mg/ml) or in water (up to at least 20 mg/ml)
Physical Properties:
Yellow solid
Purity:
98% by HPLC
NMR (Conforms)
Storage Temperature:
-20°C (des.)
Stability:
Stable for 1 year as supplied. Solutions in DMSO or distilled water may be stored at -20°C for up to 3 months.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

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