SI-2
- CAS No.
- 380537-35-9
- Chemical Name:
- SI-2
- Synonyms
- SI-2;(E)-SI-2;(E)SI2,(E) SI 2;(E)-SI-2, 10 mM in DMSO;1-Methyl-N-[(E)-1-pyridin-2-ylethylideneamino]benzimidazol-2-amine;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
- TDS File:
- TDS
| Product description | Number | Pack Size | Price |
| SI-2 ≥98% (HPLC) | SML1762 | 25MG | $434 |
| SI-2 ≥98% (HPLC) | SML1762 | 5MG | $99.5 |
| SI-2 ≥98% | 19565 | 1mg | $49 |
| SI-2 ≥98% | 19565 | 5mg | $178 |
| SI-2 ≥98% | 19565 | 10mg | $329 |
| 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. |
| SMILES | C/C(C1=CC=CC=N1)=N\NC2=NC3=C(C=CC=C3)N2C |
| UNSPSC Code | 12352200 |
| NACRES | NA.77 |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
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|---|---|---|---|---|---|---|---|---|---|---|
| Signal word | Warning | |||||||||
| Hazard statements | H315-H319 | |||||||||
| Precautionary statements | P305+P351+P338 | |||||||||
| WGK Germany | WGK 3 | |||||||||
| Storage Class | 11 - Combustible Solids | |||||||||
| Hazard Classifications | Eye Irrit. 2 Skin Irrit. 2 |
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| NFPA 704 |
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SI-2 price More Price(16)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Sigma-Aldrich | SML1762 | SI-2 ≥98% (HPLC) | 380537-35-9 | 25MG | $434 | 2026-04-30 | Buy |
| Sigma-Aldrich | SML1762 | SI-2 ≥98% (HPLC) | 380537-35-9 | 5MG | $99.5 | 2025-07-31 | Buy |
| Cayman Chemical | 19565 | SI-2 ≥98% | 380537-35-9 | 1mg | $49 | 2026-04-30 | Buy |
| Cayman Chemical | 19565 | SI-2 ≥98% | 380537-35-9 | 5mg | $178 | 2026-04-30 | Buy |
| Cayman Chemical | 19565 | SI-2 ≥98% | 380537-35-9 | 10mg | $329 | 2026-04-30 | Buy |
SI-2 Chemical Properties,Uses,Production
Description
SI-2 (380537-35-9) is a potent inhibitor of steroid receptor coactivator-3 (SRC-3).1It blocks MDA-MB-468 cell growth with an IC50= 3.4 nM without effecting normal cells.1It 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.2CSC markers CD44+/CD24-/1oand 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 micein 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] XIANZHOU SONG. Development of potent small-molecule inhibitors to drug the undruggable steroid receptor coactivator-3.[J]. Proceedings of the National Academy of Sciences of the United States of America, 2016, 113 18: 4970-4975. DOI:10.1073/pnas.1604274113
[2] AARTI D ROHIRA. Targeting SRC Coactivators Blocks the Tumor-Initiating Capacity of Cancer Stem-like Cells.[J]. Cancer research, 2017, 77 16: 4293-4304. DOI:10.1158/0008-5472.can-16-2982
[3] THU H TRUONG. Cancer Stem Cell Phenotypes in ER+ Breast Cancer Models Are Promoted by PELP1/AIB1 Complexes.[J]. Molecular Cancer Research, 2018, 16 4: 707-719. DOI:10.1158/1541-7786.mcr-17-0598
SI-2 Preparation Products And Raw materials
Raw materials
Preparation Products
SI-2 Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| TargetMol Chemicals Inc. | +1-781-999-5354; +17819995354 | marketing@targetmol.com | United States | 32467 | 58 |
| Career Henan Chemica Co | +86-0371-86658258 +8613203830695 | laboratory@coreychem.com | China | 30227 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354; | support@targetmol.com | United States | 39040 | 58 |
| Sigma-Aldrich | 021-61415566 800-8193336 | orderCN@merckgroup.com | China | 51395 | 80 |
| Shanghai EFE Biological Technology Co., Ltd. | 021-65675885 18964387627 | info@efebio.com | China | 9803 | 58 |
| Shanghai Hongye Biotechnology Co. Ltd | 400-9205774 | sales@glpbio.cn | China | 6777 | 58 |
| ChemeGen(Shanghai) Biotechnology Co.,Ltd. | 18818260767 | sales@chemegen.com | China | 11218 | 58 |
| MedBioPharmaceutical Technology Inc | 021-69568360 18916172912 | order@med-bio.cn | China | 8140 | 58 |
| Energy Chemical | 021-58432009 400-005-6266 | marketing@energy-chemical.com | China | 44918 | 58 |
| TargetMol Chemicals Inc. | 4008200310 | marketing@tsbiochem.com | China | 24960 | 58 |
