S55746 (BCL-201)
S55746 (BCL-201) Basic information
- Product Name:
- S55746 (BCL-201)
- Synonyms:
-
- S55746 (BCL-201)
- S55746 hydrochloride
- S55746 hydrochloride (Synonyms: BLC201 (hydrochloride))
- S55746 hydrochloride (BLC201 (hydrochloride))
- BLC201 (hydrochloride)
- S55746 hydrochloride,S-55746 hydrochloride
- CAS:
- 1448525-91-4
- MF:
- C43H43ClN4O6
- MW:
- 747.29
- Mol File:
- 1448525-91-4.mol
S55746 (BCL-201) Chemical Properties
- storage temp.
- Store at -20°C
- solubility
- Soluble in DMSO
- form
- Solid
- color
- White to yellow
S55746 (BCL-201) Usage And Synthesis
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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