1. Others
  2. Others
  3. SI-2 hydrochloride

SI-2 hydrochloride  (Synonyms: EPH 116 hydrochloride)

Cat. No.: HY-101447A Purity: 99.79%
COA Handling Instructions

SI-2 (EPH 116 hydrochloride) is a highly promising SRC-3 inhibitor (PPI), with IC50 values of 3-20 nM for breast cancer cell death. SI-2 (EPH 116 hydrochloride) has a much improved toxicity and pharmacokinetic profile, with acceptable oral availability.

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

SI-2 hydrochloride Chemical Structure

SI-2 hydrochloride Chemical Structure

CAS No. : 1992052-49-9

Size Price Stock Quantity
Free Sample (0.1 - 0.5 mg)   Apply Now  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 121 In-stock
Solution
10 mM * 1 mL in DMSO USD 121 In-stock
Solid
5 mg USD 110 In-stock
10 mg USD 170 In-stock
50 mg USD 550 In-stock
100 mg USD 850 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of SI-2 hydrochloride:

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

SI-2 (EPH 116 hydrochloride) is a highly promising SRC-3 inhibitor (PPI), with IC50 values of 3-20 nM for breast cancer cell death. SI-2 (EPH 116 hydrochloride) has a much improved toxicity and pharmacokinetic profile, with acceptable oral availability[1].

IC50 & Target

IC50:3-20 nM (breast cancer cell death)[1].

In Vitro

SI-2 selectively reduce the transcriptional activities and the protein concentrations of SRC-3 in cells through direct physical interactions with SRC-3[1].
? SI-2 selectively induces breast cancer cell death with IC50 values in the low nanomolar range (3-20 nM), but not affect normal cell viability[1].
? SI-2 (100 nM) decreases cell motility, invasion, and tumor metastasis in MDAMB-468 cells[1].

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

Cell Viability Assay[1].

Cell Line: MDA-MB-468 cells.
Concentration: 100 nM.
Incubation Time: 12 hours.
Result: Significantly reduced the motility of cancer cells.

Western Blot Analysis[1].

Cell Line: MDAMB-468 cells.
Concentration: 0-200 nM.
Incubation Time: 24 hours.
Result: Significantly reduced SRC-3 protein levels. Did not decrease the SRC-3 mRNA level.

Western Blot Analysis[1].

Cell Line: Cancer cells.
Concentration: 0-200 nM.
Incubation Time: 24 hours.
Result: Caused PARP cleavage.
In Vivo

SI-2 causes minimal acute cardiotoxicity based on a hERG channel blocking assay and an unappreciable chronic toxicity to major organs based on histological analyses[1].
? SI-2 is a drug-like molecule and meets all of the criteria of Lipinski’s rule[1].

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

Animal Model: MDA-MB-468 breast cancer mouse model[1].
Dosage: 2 mg/kg.
Administration: Twice daily for 5 weeks (Vehicle, PBS).
Result: Significantly inhibit tumor growth.
SRC-3 levels in SI-2–treated tumor tissues were significantly lower than the PBS treated control group.
Animal Model: CD1 mice[1].
Dosage: 20 mg/kg (Pharmacokinetic Analysis).
Administration: Intraperitoneal administration once.
Result: T1/2 = 1 h, Cmax of 3.0 μM, and the time to reach the maximum plasma concentration tmax of 0.25 h.
SI-2 only degrades slightly (less than 5%) at pH 1.6 and 3.0 within 6 h, and is stable in buffers with pH ≥ 5.
Molecular Weight

301.77

Formula

C15H16ClN5

CAS No.
Appearance

Solid

Color

Pink to red

SMILES

CN1C(N/N=C(C)/C2=CC=CC=N2)=NC3=CC=CC=C13.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 5 mg/mL (16.57 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.3138 mL 16.5689 mL 33.1378 mL
5 mM 0.6628 mL 3.3138 mL 6.6276 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.3138 mL 16.5689 mL 33.1378 mL 82.8446 mL
5 mM 0.6628 mL 3.3138 mL 6.6276 mL 16.5689 mL
10 mM 0.3314 mL 1.6569 mL 3.3138 mL 8.2845 mL
15 mM 0.2209 mL 1.1046 mL 2.2092 mL 5.5230 mL
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

SI-2 hydrochloride Related Classifications

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.

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
SI-2 hydrochloride
Cat. No.:
HY-101447A
Quantity:
MCE Japan Authorized Agent: