SGI-1776 FREE BASE
SGI-1776 free base
CAS: 1025065-69-3
Molecular Formula: C20H22F3N5O
SGI-1776 FREE BASE - Names and Identifiers
SGI-1776 FREE BASE - Physico-chemical Properties
| Molecular Formula | C20H22F3N5O |
| Molar Mass | 405.42 |
| Density | 1.37 |
| Appearance | Solid |
| pKa | 9.22±0.10(Predicted) |
| Storage Condition | -20℃ |
| Use | SGI-1776 free base is a new, ATP-competitive Pim1 inhibitor with an IC50 of 7 nM, which is 50 and 10 times more selective than Pim2 and Pim3, respectively. It is also effective on Flt3 and haspin. |
| In vitro study | In addition to Pim, SGI-1776 was also effective at FLT3 (IC50 = 44nm). SGI-1776 treatment of AML cells induces apoptosis in a concentration-dependent manner. SGI-1776 acts on AML primary cells, is toxic, and results in a Mcl-1 protein reduction. SGI-1776 treatment of CLL cells induced apoptosis in a dose-dependent manner. SGI-1776 acts on CLL, inducing apoptosis, and the mechanism of action involves a Mcl-1 reduction. Induction of apoptosis, accompanied by inhibition of RNA synthesis, was observed in SGI-1776 treated CLL cells. In vitro, SGI-1776 was toxic with a mean relative IC50 value of 3.1 mM. In contrast, SGI-1776 induced an intact subcutaneous MV4;11 response. |
| In vivo study | SGI-1776 is effective in a MV-4-11 tumor-bearing mouse model. SGI-1776 acts on leukemia and solid tumor cell lines and has preclinical activity with IC50 of 0.005-11.68 mM. In vivo, SGI-1776 acts on 9 out of 31 solid xenografts and 1 out of 8 ALL xenografts, significantly inducing differentiation in the EFS profile. |
SGI-1776 FREE BASE - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.467 ml | 12.333 ml | 24.666 ml |
| 5 mM | 0.493 ml | 2.467 ml | 4.933 ml |
| 10 mM | 0.247 ml | 1.233 ml | 2.467 ml |
| 5 mM | 0.049 ml | 0.247 ml | 0.493 ml |
Last Update：2024-01-02 23:10:35
SGI-1776 FREE BASE - Reference Information
| biological activity | SGI-1776 free base is a novel, ATP-competitive Pim1 inhibitor, the IC50 in the cell-free assay is 7 nM, which is 50 and 10 times more selective than Pim2 and Pim3, respectively, and is also effective for Flt3 and haspin. SGI-1776 can induce apoptosis and autophagy. Phase 1. |
| Target | TargetValue Pim1 (Cell-free assay) 7 nM FLT3 (Cell-free assay) 44 nM Pim3 (Cell-free assay) 69 nM Pim2 (Cell-free assay) 363 nM |
| Target | Value |
| Pim1 (Cell-free assay) | 7 nM |
| FLT3 (Cell-free assay) | 44 nM |
| Pim3 (Cell-free assay) | 69 nM |
| Pim2 (Cell-free assay) | 363 nM |
| in vitro study | In addition to Pim, SGI-1776 was also effective at FLT3 (IC50 = 44nm). SGI-1776 treatment of AML cells induces apoptosis in a concentration-dependent manner. SGI-1776 acts on AML primary cells, is toxic, and results in a Mcl-1 protein reduction. SGI-1776 treatment of CLL cells induced apoptosis in a dose-dependent manner. SGI-1776 acts on CLL, inducing apoptosis, and the mechanism of action involves a Mcl-1 reduction. Induction of apoptosis, accompanied by inhibition of RNA synthesis, was observed in SGI-1776 treated CLL cells. In vitro, SGI-1776 was toxic with a mean relative IC50 value of 3.1 mM. In contrast, SGI-1776 induced an intact subcutaneous MV4;11 response. |
| in vivo study | SGI-1776 is effective in a MV-4-11 tumor-bearing mouse model. SGI-1776 acts on leukemia and solid tumor cell lines and has preclinical activity with IC50 of 0.005-11.68 mM. In vivo, SGI-1776 acts on 9 out of 31 solid xenografts and 1 out of 8 ALL xenografts, significantly inducing differentiation in the EFS profile. |
Last Update：2024-04-10 22:29:15
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Product Name: SGI-1776 free base Visit Supplier Webpage Request for quotationCAS: 1025065-69-3
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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