Bulk Inquiry
SHP099
- Soluble in DMSO
- MF: C16H19Cl2N5
- MW: 352.26
Description
Highly potent, selective and orally bioavailable SHP2 inhibitor (IC50 value 0.071 μM) that stabilizes SHP2 in an auto-inhibited conformation. SHP099 potently inhibits ERK phosphorylation and the growth of cancer cell lines that have alterations in RTKs or other tyrosine kinases such as the Janus kinases JAK1 and JAK2. SHP099 showed no detectable activity against a panel of 21 phosphatases and 66 kinases (including the closest homologue SHP1), and only had modest activity against 5HT3 when profiled against a preclinical safety pharmacology panel representing 49 common adverse drug reaction targets.
More Information
| Parent CAS No. | 1801747-42-1 |
|---|---|
| Chemical Name | 6-(4-amino-4-methylpiperidin-1-yl)-3-(2,3-dichlorophenyl)pyrazin-2-amine |
| SMILES | C1(N)=NC(N2CCC(N)(C)CC2)=CN=C1C1=CC=CC(Cl)=C1Cl |
| MFCD | N.A. |
| InChi | InChI=1S/C16H19Cl2N5/c1-16(20)5-7-23(8-6-16)12-9-21-14(15(19)22-12)10-3-2-4-11(17)13(10)18/h2-4,9H,5-8,20H2,1H3,(H2,19,22) |
| InChiKey | YGUFCDOEKKVKJK-UHFFFAOYSA-N |
| CID | 118238298 |
| Short Description | SHP2 inhibitor |
References
- J Garcia Fortanet et al. Allosteric Inhibition of SHP2: Identification of a Potent, Selective, and Orally Efficacious Phosphatase Inhibitor. J Med Chem. 2016 Sep 8;59(17):7773-82.
- YN Chen et al. Allosteric inhibition of SHP2 phosphatase inhibits cancers driven by receptor tyrosine kinases. Nature. 2016 Jul 7;535(7610):148-52.
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