1. Apoptosis
  2. Bcl-2 Family

S55746 (Synonyms: BLC201)

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

S55746 is an orally active, selective and potent BCL-2 inhibitor, with a Ki of 1.3 nM.

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 610 In-stock
Estimated Time of Arrival: December 31
5 mg USD 390 In-stock
Estimated Time of Arrival: December 31
10 mg USD 590 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1200 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1950 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2950 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

S55746 is an orally active, selective and potent BCL-2 inhibitor, with a Ki of 1.3 nM.

IC50 & Target

Bcl-2

1.3 nM (Ki)

In Vitro

S55746 is a potent inhibitor of BCL-2 (Ki=1.3 nM). S55746 potently induces RS4;11 cell killing after 72 h of treatment with an IC50 of 71.6 nM. Interestingly, S55746 exhibits a much weaker activity in H146 (IC50=1.7 μM), a BCL-XL-dependent cell line, which expresses a low level of BCL-2 and high level of BCL-XL whereas ABT-263, which targets BCL-2 and BCL-XL, induces equivalent cell killing in both RS4;11 and H146 (41.5 nM and 49.7 nM, respectively). S55746-induced apoptosis in RS4;11 is mediated in part by the BAX effector protein since PARP cleavage is markedly inhibited in BAX-deficient RS4;11 cells. S55746 is shown to strongly induce apoptosis in BCL-2-dependent FL5.12 cells with a minor effect in BCL-XL-dependent FL5.12 cells[1].

In Vivo

Caspase-3 activity after S55746 treatment at 25 and 100 mg/kg is about 11 and 28 times higher than in vehicle-treated animals, respectively. Antitumor activity of S55746 is then evaluated in RS4;11 and Toledo models, two models that display different in vitro sensitivities towards S55746 (71.6 nM in RS4;11 vs 401 nM in Toledo). In RS4;11 bearing SCID mice, daily oral gavage treatment of S55746 for 7 consecutive days induce significant anti-tumor activity compared to untreated animals. Seventeen days after beginning of treatment at 25 mg/kg, 50 mg/kg and 100 mg/kg, tumor growth inhibition is 67.1, 16.3 and −93.8 T/C respectively, with complete regression observed in all animals treated at 100 mg/kg. Efficacy of S55746 is also assessed in Toledo bearing mice. After 21 days of treatment, S55746 induces a significant tumor growth inhibition either at 200 or 300 mg/kg (13% and 2% T/C, respectively; p<0.05). In this model, S55746 and ABT-199 show similar anti-tumor efficacy[1].

Clinical Trial
Solvent & Solubility
In Vitro: 

H2O

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.
References
Animal Administration
[1]

Mice[1]
Experiments are performed in SCID/beige female mice. RS4;11 Acute Lymphoblastic Leukemia cell lines and human cell lines are used. For each experiment, female SCID/beige mice are implanted subcutaneously with 3×106 Toledo or RS4;11. Body weights are recorded and tumors are measured with digital calipers twice to three times a week. When tumors reached approximately 200 mm3 for efficacy studies or 300 mm3 for pharmacodynamics studies, mice are randomized. S55746 is formulated in PEG300/EtOH/water (40/10/50). Mice are treated via oral gavage at 10 mL/kg with different doses (e.g., S55746: 20, 50, 100 mg/kg)[1].

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

References
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

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
S55746
Cat. No.:
HY-117288
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S55746

Cat. No.: HY-117288