SHP099 | SHP2 inhibitor
NMR (Conforms)
Available Options
| Size : | Price | Quantity | |
|---|---|---|---|
| 5 mg | $75.00 | ||
| 25 mg | $260.00 |
SHP099 (1801747-42-4) 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, in combination 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
NMR (Conforms)
Safety Data Sheet:
Product Data Sheet:
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. 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
SHP099 (1801747-42-4) 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, in combination 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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Focus Biomolecules • Plymouth Meeting, PA USA • 1-855-FOCUS21
Focus Biomolecules
Plymouth Meeting, PA USA
1-855-FOCUS21
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