SI-2
- CAS No.
- 380537-35-9
- Chemical Name:
- SI-2
- Synonyms
- SI-2;(E)-SI-2;(E)SI2,(E) SI 2;1-(2-pyridinyl)-, 2-(1-methyl-1H-benzimidazol-2-yl)hydrazone, (1E)-;Ethanone, 1-(2-pyridinyl)-, 2-(1-methyl-1H-benzimidazol-2-yl)hydrazone, (1E)-
- CBNumber:
- CB33152741
- Molecular Formula:
- C15H15N5
- Molecular Weight:
- 265.313
- MDL Number:
- MFCD30537542
- MOL File:
- 380537-35-9.mol
- MSDS File:
- SDS
| Boiling point | 459.9±37.0 °C(Predicted) |
|---|---|
| Density | 1.22±0.1 g/cm3(Predicted) |
| storage temp. | 2-8°C |
| solubility | Soluble in DMSO (up to 20 mg/ml). |
| pka | 11.05±0.70(Predicted) |
| form | solid |
| color | Pale orange |
| Stability | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 1 month. |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Signal word | Warning | |||||||||
| Hazard statements | H315-H319 | |||||||||
| Precautionary statements | P305+P351+P338 | |||||||||
| NFPA 704 |
|
SI-2 price More Price(12)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Sigma-Aldrich | SML1762 | SI-2 ≥98% (HPLC) | 380537-35-9 | 5MG | $107 | 2023-06-20 | Buy |
| Sigma-Aldrich | SML1762 | SI-2 ≥98% (HPLC) | 380537-35-9 | 25MG | $434 | 2023-06-20 | Buy |
| Cayman Chemical | 19565 | SI-2 ≥98% | 380537-35-9 | 1mg | $44 | 2024-03-01 | Buy |
| Cayman Chemical | 19565 | SI-2 ≥98% | 380537-35-9 | 5mg | $161 | 2024-03-01 | Buy |
| Cayman Chemical | 19565 | SI-2 ≥98% | 380537-35-9 | 10mg | $299 | 2024-03-01 | Buy |
SI-2 Chemical Properties,Uses,Production
Description
SI-2 (380537-35-9) is a potent inhibitor of steroid receptor coactivator-3 (SRC-3).1?It blocks MDA-MB-468 cell growth with an IC50?= 3.4 nM without effecting normal cells.1?It significantly inhibited breast cancer cell growth in an orthotopic MDA-MD-468 mouse model. Treatment of MCF-7 or triple negative MDA-MB-231 cells with SI-2 resulted in inhibition of proliferation and breast cancer stem cell (CSC) tumorsphere formation.2?CSC markers CD44+/CD24-/1o?and aldehyde dehydrogenase (ALDH) were also reduced indicating that SI-2 can selectively interfere with the TIC/CSC state in breast cancer cells.2,3
Uses
SI-2 is an inhibitor of steroid receptor coactivator-3 (SRC-3). Induces cell death in verious breast cancer cells.
Biochem/physiol Actions
SI-2 targets the receptor-interacting domain (RID) of steroid receptor coactivators (SRCs) and suppresses cellular transcriptional activity (Effec. conc. >/= 5 nM in cell-based SRC-1, SRC-2, and SRC-3 reporter assays) by downregulating SRCs protein, but not transcript level (Effec. conc. >/= 12.5 nM against SRC-3, >/= 25 nM against SRC-1 and SCR-2 in MDA-MB-468 culture). SI-2 is cytotoxic to breast cancer cultures (IC50?= 1.5 nM/BT-474, 3.4 nM/MDA-MB-468, 22 nM/MCF-7), but not to normal hepatocytes even at 500 nM concentration. SI-2 is reported to be orally available in mice and, when administered intraperitoneally (2 mg/kg b.i.d.), effectively suppress MDA-MB-468-derived tumor expansion in mice?in vivowith good pharmacokinetics (Cmax?= 30 μM,?tmax?= 0.25 h,?t1/2?= 1.0 h; 20 mg/kg i.p.) and no apparent adverse effects to the animals.
References
1) Song?et al.?(2016),?Development of potent small-molecule inhibitors to drug the undruggable steroid receptor coactivator-3; Proc. Natl. Acad. Sci. USA?113?4970 2) Rohira?et al.?(2017),?Targeting SRC Coactivators Blocks the Tumor-Initiating Capacity of Cancer Stem-like Cells; Cancer Res.?77?4293 3) Truong?et al.?(2018),?Cancer Stem Cell Phenotypes in ER+ Breast Cancer Models are Promoted by PELP/AIB1 Complexes; Mol. Cancer Res.?16?707
SI-2 Preparation Products And Raw materials
Raw materials
Preparation Products
SI-2 Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| Career Henan Chemica Co | +86-0371-86658258 15093356674; | laboratory@coreychem.com | China | 30255 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354 | support@targetmol.com | United States | 19973 | 58 |
| Sigma-Aldrich | 021-61415566 800-8193336 | orderCN@merckgroup.com | China | 51471 | 80 |
| Shanghai Hongye Biotechnology Co. Ltd | 400-9205774 | sales@glpbio.cn | China | 6870 | 58 |
| DC Chemicals | 021-58447131 13564518121 | sales@dcchemicals.com | China | 9414 | 58 |
| ChemeGen(Shanghai) Biotechnology Co.,Ltd. | 18818260767 | sales@chemegen.com | China | 11289 | 58 |
| MedBioPharmaceutical Technology Inc | 021-69568360 18916172912 | order@med-bio.cn | China | 8141 | 58 |
| Energy Chemical | 021-58432009 400-005-6266 | marketing@energy-chemical.com | China | 44941 | 58 |
| TargetMol Chemicals Inc. | 4008200310 | marketing@tsbiochem.com | China | 24131 | 58 |
| Shanghai Maclean Biochemical Technology Co., LTD | 021-50706066 15221275939 | shenlinxing@macklin.cn | China | 29803 | 58 |