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  3. S55746 hydrochloride

S55746 hydrochloride  (Synonyms: BCL201 hydrochloride)

Cat. No.: HY-117288A Purity: 99.66%
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S55746 hydrochloride (BCL201 hydrochloride) is a potent, orally active and selective BCL-2 inhibitor, with a Ki of 1.3 nM and a Kd of 3.9 nM. S55746 hydrochloride (BCL201 hydrochloride) has antitumor activity with low toxicity.

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

S55746 hydrochloride Chemical Structure

S55746 hydrochloride Chemical Structure

CAS No. : 1448525-91-4

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of S55746 hydrochloride:

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  • Biological Activity

  • Purity & Documentation

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Description

S55746 hydrochloride (BCL201 hydrochloride) is a potent, orally active and selective BCL-2 inhibitor, with a Ki of 1.3 nM and a Kd of 3.9 nM. S55746 hydrochloride (BCL201 hydrochloride) has antitumor activity with low toxicity[1].

IC50 & Target[1]

Bcl-2

1.3 nM (Ki)

Bcl-xL

520 nM (Ki)

Bcl-2

3.9 nM (Kd)

Bcl-xL

186 nM (Kd)

In Vitro

S55746 (0-1 μM) potently and selectively induces cell death[1].
S55746 selectively induces apoptosis through BCL-2 inhibition in a BAX/BAK-dependent manner[1].

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

Western Blot Analysis[1]

Cell Line: H146 and RS4;11 cell lines.
Concentration: 0, 0.1, 0.3 and 1 μM.
Incubation Time: 72 hours.
Result: Potently induced RS4;11 cell killing after 72 h of treatment with an IC50 of 71.6 nM.
In Vivo

S55746 is a highly efficacious and well-tolerated (even at doses up to 300 mg/kg) orally active BCL-2 inhibitor [1].
S55746 (20-100 mg/kg, p.o.) inhibits xenograft growth in RS4;11 and Toledo models time- and dose-dependently[1].

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

Animal Model: Female SCID/beige mice implanted subcutaneously with 3×106 Toledo or RS4;11[1].
Dosage: 20, 50, 100 mg/kg.
Administration: Oral gavage daily for 7 consecutive days.
Result: Induced significant anti-tumor activity time- and dose-dependently.
Animal Model: SCID/beige female mice with RS4;11 tumor xenografts[1].
Dosage: 25 and 100 mg/kg.
Administration: Single oral gavage treatment.
Result: Did not induce platelet loss in vivo at 25 and 100 mg/kg.
Clinical Trial
Molecular Weight

747.28

Formula

C43H43ClN4O6

CAS No.
Appearance

Solid

Color

White to yellow

SMILES

O=C(C1=C2CCCCN2C(C3=C(C(N4CC5=C(C=CC=C5)C[C@H]4CN6CCOCC6)=O)C=C(OCO7)C7=C3)=C1)N(C8=CC=C(O)C=C8)C9=CC=CC=C9.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 200 mg/mL (267.64 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 1.3382 mL 6.6909 mL 13.3819 mL
5 mM 0.2676 mL 1.3382 mL 2.6764 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 (stored under nitrogen). 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
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 5 mg/mL (6.69 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 5 mg/mL (6.69 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
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 (stored under nitrogen). 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 1.3382 mL 6.6909 mL 13.3819 mL 33.4547 mL
5 mM 0.2676 mL 1.3382 mL 2.6764 mL 6.6909 mL
10 mM 0.1338 mL 0.6691 mL 1.3382 mL 3.3455 mL
15 mM 0.0892 mL 0.4461 mL 0.8921 mL 2.2303 mL
20 mM 0.0669 mL 0.3345 mL 0.6691 mL 1.6727 mL
25 mM 0.0535 mL 0.2676 mL 0.5353 mL 1.3382 mL
30 mM 0.0446 mL 0.2230 mL 0.4461 mL 1.1152 mL
40 mM 0.0335 mL 0.1673 mL 0.3345 mL 0.8364 mL
50 mM 0.0268 mL 0.1338 mL 0.2676 mL 0.6691 mL
60 mM 0.0223 mL 0.1115 mL 0.2230 mL 0.5576 mL
80 mM 0.0167 mL 0.0836 mL 0.1673 mL 0.4182 mL
100 mM 0.0134 mL 0.0669 mL 0.1338 mL 0.3345 mL
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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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S55746 hydrochloride
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