Identification | Back Directory | [Name]
S55746 (BCL-201) | [CAS]
1448525-91-4 | [Synonyms]
S55746 (BCL-201) S55746 hydrochloride BLC201 (hydrochloride) S55746 hydrochloride (BLC201 (hydrochloride)) S55746 hydrochloride (Synonyms: BLC201 (hydrochloride)) | [Molecular Formula]
C43H43ClN4O6 | [MOL File]
1448525-91-4.mol | [Molecular Weight]
747.29 |
Hazard Information | Back Directory | [Description]
S55746 hydrochloride is a potent, orally active and selective BCL-2 inhibitor with antitumor activity with low toxicity. | [Uses]
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]. | [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. |
| [IC 50]
Bcl-2: 1.3 nM (Ki); Bcl-xL: 520 nM (Ki); Bcl-2: 3.9 nM (Kd); Bcl-xL: 186 nM (Kd) | [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. DOI:10.18632/oncotarget.24744 |
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Company Name: |
cjbscvictory
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Tel: |
13348960310 |
Website: |
https://www.weikeqi-biotech.com/ |
Company Name: |
Biorbyt Ltd.
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Tel: |
+44 (0)1223 859 353 |
Website: |
http://www.biorbyt.com |
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