CS-786
NVP-HSP990(HSP990)
CAS: 934343-74-5
Molecular Formula: C20H18FN5O2
CS-786 - Names and Identifiers
CS-786 - Physico-chemical Properties
| Molecular Formula | C20H18FN5O2 |
| Molar Mass | 379.39 |
| Density | 1.332 |
| Storage Condition | 2-8℃ |
| In vitro study | NVP-HSP990 is based on the 2-amino -4-methyl -7, 8-dihydropyridine [4,3-d] pyrimidin-5 (6H)-One backbone, which is structurally different from other known HSP90 inhibitors. NVP-HSP990 binds to the N-terminus of the ATP-binding domain of HSP90. NVP-HSP990 has IC50 values in units of millimolar order for the three HSP90 subtypes (HSP90α, HSP90β, and GRP94) and an IC50 value of 320 nM for the fourth (TRAP-1), it is selective for unrelated enzymes, receptors and kinases. NVP-HSP990 dissociates HSP90-p23 of the complex, depletes client protein c-Met, and induces Hsp70 in c-Met magnified GTL-16 gastric tumor cells. NVP-HSP990 effectively inhibits the growth of human cell lines and various types of primary tumors. NVP-HSP990 showed a dose and time dependent effect on HSP90 client proteins. NVP-HSP990 inhibits the proliferation of all GIC line glioma tumor initiating cells (GICs) with IC50 values ranging from approximately 10 to 500 nM. Olig2 is a functional marker associated with cell differentiation, and in response to the associated NVP-HSP990, NVP-HSP990 attenuated cell proliferation in the Olig2 high GIC line. In addition, NVP-HSP990 disrupted cell cycle control mechanisms by reducing CDK2 and CDK4 and increasing apoptosis-related molecules. |
| In vivo study | NVP-HSP990 showed similar pharmaceutical and pharmacological properties of the drug, with high oral biological activity. A single oral dose of 15 mg/kg GTL-16 induced sustained NVP-HSP990 downregulation and Hsp70 upregulation in a c-Met xenograft model. In repeat-dose studies, NVP-HSP990 treatment resulted in GTL-16 tumor growth inhibition, which also resulted in growth inhibition in other human tumor transplantation models driven by well-defined oncogenic HSP90 client proteins. |
CS-786 - Risk and Safety
| HS Code | 29339900 |
CS-786 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.636 ml | 13.179 ml | 26.358 ml |
| 5 mM | 0.527 ml | 2.636 ml | 5.272 ml |
| 10 mM | 0.264 ml | 1.318 ml | 2.636 ml |
| 5 mM | 0.053 ml | 0.264 ml | 0.527 ml |
Last Update：2024-01-02 23:10:35
CS-786 - Reference Information
| biological activity | HSP990 (NVP-HSP990) is a new and effective selective HSP90 inhibitor with IC50 of 0.6 nM and 0.8 nM for HSP90α/β respectively. NVP-HSP990 can induce cell cycle arrest and apoptosis. |
| target | TargetValue HSP90α (Cell-free assay) 0.6 nM HSP90β (Cell-free assay) 0.8 nM |
| Target | Value |
| HSP90α (Cell-free assay) | 0.6 nM |
| HSP90β (Cell-free assay) | 0.8 nM |
| in vitro study | NVP-HSP990 is based on 2-amino -4-methyl -7, 8-dihydropyridine [4,3-d] pyrimidine -5(6H)-ketone skeleton, and its structure is different from other known HSP90 inhibitors. NVP-HSP990 binds to the N-terminal of the ATP binding domain of HSP90. The NVP-HSP990 has IC50 values in the unit number millimolar order for the three HSP90 subtypes (HSP90α, HSP90β, and GRP94) and 320 nM for the fourth (TRAP-1), which is selective for unrelated enzymes, receptors, and kinases. NVP-HSP990 frees the HSP90-p23 complex, depletes the client protein c-Met, and induces Hsp70 in c-Met-amplified GTL-16 gastric tumor cells. NVP-HSP990 effectively inhibit the growth of human cell lines and various types of primary tumors. NVP-HSP990 showed a dose-and time-dependent effect on HSP90 client protein. NVP-HSP990 inhibit the proliferation of tumor initiation cells (GIC) of all GIC lines of glioma, the IC50 value ranges from about 10 to 500 nM. Olig2 is a functional marker related to cell differentiation, and in response to the associated NVP-HSP990, cell proliferation is NVP-HSP990 attenuated in GIC lines with high Olig2. In addition, NVP-HSP990 destroy the cell cycle control mechanism by reducing CDK2 and CDK4 and increasing apoptosis-related molecules. |
| in vivo research | NVP-HSP990 show pharmaceutical and pharmacological properties similar to drugs and have high oral biological activity. In a GTL-16 xenograft model, a single oral administration of 15 mg/kg NVP-HSP990 induced sustained c-Met downregulation and Hsp70 upregulation. In repeated dose studies, NVP-HSP990 treatment resulted in GTL-16 tumor growth inhibition, which also resulted in growth inhibition on other well-defined oncogenic HSP90 client protein-driven human tumor transplantation models. |
Last Update：2024-04-09 21:04:16
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Spot supply
Product Name: NVP-HSP990(HSP990) Visit Supplier Webpage Request for quotationCAS: 934343-74-5
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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