1. Protein Tyrosine Kinase/RTK
  2. Src
  3. 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.

For research use only. We do not sell to patients.

SRC-3-IN-1

SRC-3-IN-1 Chemical Structure

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Description

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[1].

Cellular Effect
Cell Line Type Value Description References
BT-474 IC50
1 nM
Compound: SI-10 (6p)
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
[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
[PMID: 38551814]
LNCaP IC50
11 nM
Compound: SI-10 (6p)
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
[PMID: 38551814]
MCF7 IC50
3.3 nM
Compound: SI-10 (6p)
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
[PMID: 38551814]
MDA-MB-468 IC50
32 nM
Compound: SI-10 (6p)
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
[PMID: 38551814]
PANC-1 IC50
8 nM
Compound: SI-10 (6p)
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
[PMID: 38551814]
In Vitro

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.

Cell Viability Assay[1]

Cell Line: Panc-1, HPAC, Mpanc-96, MDA-MB-468, MCF-7, BT-474 and LNCaP cell lines
Concentration:
Incubation Time: 72 h
Result: Exhibited very potent cytotoxicity against these cell lines, with IC50 values ranging from 1 to 32 nM
In Vivo

SRC-3-IN-1(50, 100 mg/kg, po.; everyday for 4 weeks) do not cause any loss of body weight[1].
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

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: xenograft prostate cancer mouse model[1]
Dosage: 10 mg/kg
Administration: i.p.
Result: Resulted in a substantial inhibition of tumor growth after only 1 week and exhibited a remarkable reduction in tumor growth by more than 65% compared to the vehicle after 4 weeks.
Molecular Weight

302.28

Formula

C14H12F2N6

SMILES

C/C(C1=NC=CC=N1)=N\N=C2N(C3=C(N\2)C=C(F)C(F)=C3)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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SRC-3-IN-1 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
SRC-3-IN-1
Cat. No.:
HY-163468
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