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

S55746 hydrochloride (Synonyms: BLC201 (hydrochloride))

Cat. No.: HY-117288A
Handling Instructions

S55746 hydrochloride (BLC201 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 (BLC201 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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Description

S55746 hydrochloride (BLC201 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 (BLC201 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].

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

747.28

Formula

C₄₃H₄₃ClN₄O₆

CAS No.

1448525-91-4

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.Cl

Shipping

Room temperature in continental US; may vary elsewhere

Storage

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

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S55746 hydrochloride
Cat. No.:
HY-117288A
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