SHP-099
SHP099 hydrochloride
CAS: 1801747-11-4
Molecular Formula: C16H20Cl3N5
SHP-099 - Names and Identifiers
SHP-099 - Physico-chemical Properties
| Molecular Formula | C16H20Cl3N5 |
| Molar Mass | 388.72 |
| Solubility | DMSO: 4.1 mg/mL |
| Storage Condition | -20℃ |
| In vitro study | SHP099 inhibits cell proliferation (KYSE-520 cells) with an IC50 of 1.4 μm. In the phosphatase and kinase Library, SHP099 has no obvious biochemical inhibitory activity, indicating that SHP099 is selective for shp2. In addition, in Caco-2 cells, SHP099 has good solubility (solubility in the buffer of pH6.8 is more than 0.5 mM) and high permeability without obvious outflow phenomenon. SHP099 can stabilize SHP2 in a self-inhibiting conformation. It inhibits RAS-ERK signaling pathways and inhibits cancer cell proliferation driven by tyrosine kinase receptors. In preclinical preclinical safety pharmacology testing, SHP099 had only moderate activity against 5HT3 among 49 commonly used drug adverse reaction targets. SHP099 has no activity on SHP1. In MDA-MB-468 and KYSE520 cells dependent on SHP2, it can inhibit p-ERK with an IC50 of about 0.25 μm, but it has no such effect in A2058 cells. In these cells, p-AKT levels were unaffected. SHP099 inhibits the MAPK signaling pathway and cell proliferation by acting directly on SHP2 in RTK-dependent cells. |
| In vivo study | SHP099 had good acceptable oral exposure (5 mg/kg PO, 565 μm/h) and oral bioavailability (46% F). It is a potent, selective, highly soluble, orally active SHP2 inhibitor in animal models of xenografts, it can inhibit the corresponding signal pathway in a concentration-dependent manner and has anti-tumor activity. In the KYSE520 transplanted tumor model, oral SHP099 will bring dose-dependent anti-tumor activity, well tolerated. |
SHP-099 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.573 ml | 12.863 ml | 25.725 ml |
| 5 mM | 0.515 ml | 2.573 ml | 5.145 ml |
| 10 mM | 0.257 ml | 1.286 ml | 2.573 ml |
| 5 mM | 0.051 ml | 0.257 ml | 0.515 ml |
Last Update：2024-01-02 23:10:35
SHP-099 - Reference Information
| biological activity | SHP099 is a potent, selective and orally active small-molecule SHP2 inhibitor, the IC50 was 0.071 μm and had no activity against shp1. |
| Target | Value |
| SHP-2 (Cell-free assay) | 0.07 μM |
Last Update：2024-04-10 22:29:15
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Spot supply
Product Name: SHP099 hydrochloride Visit Supplier Webpage Request for quotationCAS: 1801747-11-4
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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