[CAS NO. 1448525-91-4] S55746hydrochloride

Name: S55746hydrochloride
Brand: Arctom Scientific
SKU: AS940598

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PRODUCTS SPECIFICATIONS [1448525-91-4]

Distributor

Catalog

AS940598

Brand

Arctom Scientific

CAS

1448525-91-4

DESCRIPTION [1448525-91-4]

Overview

MDL	MFCD31746916
Molecular Weight	747.28
Molecular Formula	C43H43ClN4O6
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

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

1 Publications Citing Use of MCE

[1]Biomed Pharmacother. 2021 Jan 1;135:111213.

Summary

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

IC50 & Target

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] .

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 IC ₅₀ 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] .

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

Animal Model:	Female SCID/beige mice implanted subcutaneously with 3×10 ⁶ 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

NCT Number	Sponsor	Condition	Start Date	Phase
NCT02920697	Institut de Recherches Internationales Servier\|ADIR, a Servier Group company\|Servier	Chronic Lymphocytic Leukaemia (CLL)\|B-Cell Non-Hodgkin Lymphoma (NHL)\|Multiple Myeloma (MM)	March 2014	Phase 1
NCT02603445	Novartis Pharmaceuticals\|Novartis	Follicular Lymphoma, Mantle Cell Lymphoma	November 16, 2015	Phase 1

Appearance

Solid

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)

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
10 mM	0.1338 mL	0.6691 mL	1.3382 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

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
2.

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

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

* All of the co-solvents are available by MCE.

References

[1] Casara P, et al. S55746 is a novel orally active BCL-2 selective and potent inhibitor that impairs hematological tumor growth. Oncotarget. 2018 Apr 13;9(28):20075-20088.