SRC-3-IN-1
SRC-3-IN-1 (compound SI-10) is a steroid receptor coactivator 3 (SRC-3) inhibitor (IC50=3.3 μM). SRC-3-IN-1 has good water solubility, oral bioavailability, and improved selectivity profile. SRC-3-IN-1 can be used in prostate cancer research.
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- No. CAS: 2137490-93-6
- Fòrmula: C14H12F2N6
- Peso molecular:302.28
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Almacenamiento:
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Actividad biológica
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BT-474 | IC50 |
1 nM
Compound: SI-10 (6p)
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Cytotoxicity against human BT-474 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Cytotoxicity against human BT-474 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
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[PMID: 38551814] |
| Hepatocyte | IC50 |
>1000 nM
Compound: SI-10 (6p)
|
Cytotoxicity against CD-1 mouse Primary hepatocyte assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Cytotoxicity against CD-1 mouse Primary hepatocyte assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
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[PMID: 38551814] |
| LNCaP | IC50 |
11 nM
Compound: SI-10 (6p)
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Cytotoxicity against human LNCaP cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Cytotoxicity against human LNCaP cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
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[PMID: 38551814] |
| MCF7 | IC50 |
3.3 nM
Compound: SI-10 (6p)
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Cytotoxicity against human MCF7 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Cytotoxicity against human MCF7 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
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[PMID: 38551814] |
| MDA-MB-468 | IC50 |
32 nM
Compound: SI-10 (6p)
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Cytotoxicity against human MDA-MB-468 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Cytotoxicity against human MDA-MB-468 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
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[PMID: 38551814] |
| PANC-1 | IC50 |
8 nM
Compound: SI-10 (6p)
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Cytotoxicity against human PANC-1 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Cytotoxicity against human PANC-1 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
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[PMID: 38551814] |
SRC-3-IN-1(different concentrations, 72 h) has a high potency against various cancer cell lines[1].
SRC-3-IN-1 exhibits high selectivity away from these off-targets compared to the single digit nanomole potency[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Panc-1, HPAC, Mpanc-96, MDA-MB-468, MCF-7, BT-474 and LNCaP cell lines
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Concentration:
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Incubation Time:72 h
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Result:Exhibited very potent cytotoxicity against these cell lines, with IC50 values ranging from 1 to 32 nM
SRC-3-IN-1(10 mg/kg, ip.; everyday for 4 weeks) prolongs mouse survival compared to the vehicle control group by inhibiting tumor angiogenesis[1].
SRC-3-IN-1(10 mg/kg/day, ip.; 4 weeks) decreases the ratio of tumor area to femur area by over 50%[1].
Pharmacokinetic Analysis in CD-1 Mice[1]
| Route | Dose (mg/kg) | T1/2 (h) | Tmax (h) | Cmax (ng/mL) | AUC0_t (ng•h/mL) | Cl (L•h/kg) | F (%) |
| i.v. | 1 | 3.25 | 0.033 | 552 | 87.6 | 176 | / |
| p.o. | 10 | 9.09 | 0.25 | 89 | 477 | / | 54.4 |