1. Apoptosis
  2. Bcl-2 Family
  3. S55746

S55746 (Synonyms: BLC201)

Cat. No.: HY-117288 Purity: 98.97%
Handling Instructions

S55746 (BLC201) 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 (BLC201) has antitumor activity with low toxicity.

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

S55746 Chemical Structure

S55746 Chemical Structure

CAS No. : 1448584-12-0

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 235 In-stock
Estimated Time of Arrival: December 31
5 mg USD 150 In-stock
Estimated Time of Arrival: December 31
10 mg USD 260 In-stock
Estimated Time of Arrival: December 31
25 mg USD 550 In-stock
Estimated Time of Arrival: December 31
50 mg USD 990 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1700 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

S55746 (BLC201) 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 (BLC201) 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].

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].

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

710.82

Formula

C₄₃H₄₂N₄O₆

CAS No.

1448584-12-0

SMILES

O=C(C1=C2CCCCN2C(C3=C(C(N4CC5=C(C=CC=C5)C[[email protected]]4CN6CCOCC6)=O)C=C(OCO7)C7=C3)=C1)N(C8=CC=C(O)C=C8)C9=CC=CC=C9

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (70.34 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.4068 mL 7.0341 mL 14.0683 mL
5 mM 0.2814 mL 1.4068 mL 2.8137 mL
10 mM 0.1407 mL 0.7034 mL 1.4068 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (3.52 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (3.52 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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S55746
Cat. No.:
HY-117288
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