SI-2
SIGMA/SML1762 - ≥98% (HPLC)
Synonym: (1E)
CAS Number: 380537-35-9
Empirical Formula (Hill Notation): C15H15N5
Molecular Weight: 265.31
Linear Formula: C15H15N5
Product Type: Chemical
| assay | ≥98% (HPLC) |
| color | , light yellow to dark orange |
| form | powder |
| Quality Level | 100  |
| SMILES string | C/C(C1=CC=CC=N1)=NNC2=NC |
| solubility | DMSO: 20 mg/mL, clear |
| storage temp. | 2-8°C |
| 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. |
| Biochem/physiol Actions: | SI-2 targets the receptor-interacting domain (RID) of steroid receptor coactivators (SRCs) and suppresses cellular transcriptional activity. |
| Packaging: | 5, 25 mg in glass bottle |
| Symbol |  GHS07 |
| Signal word | Warning |
| Hazard statements | H315 - H319 |
| Precautionary statements | P305 + P351 + P338 |
| RIDADR | NONH for all modes of transport |
| WGK Germany | WGK 3 |
| Flash Point(F) | Not applicable |
| Flash Point(C) | Not applicable |
| Purity | ≥98% (HPLC) |
| Storage Temp. | 2-8°C |
| UNSPSC | 12352200 |