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S55746 hydrochloride (BLC201 hydrochloride) is a novel, potent, selective and orally bioavailable 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.
| ln Vitro |
S55746 (0-1 μM) potently and selectively triggers cell death [1]. S55746 preferentially promotes apoptosis by inhibiting BCL-2 in a BAX/BAK-dependent manner [1].
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| ln Vivo |
S55746 is an oral active BCL-2 inhibitor that is very effective and well-tolerated (even at doses up to 300 mg/kg) [1]. In the RS4;11 and Toledo models, S55746 (20–100 mg/kg, oral) suppresses xenograft growth in a dose- and time-dependent manner [1].
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: H146 and RS4; 11 cell lines. Tested Concentrations: 0, 0.1, 0.3 and 1 μM. Incubation Duration: 72 hrs (hours). Experimental Results: After 72 hrs (hours) of treatment, RS4;11 cell death was effectively induced, with an IC50 of 71.6 nM. |
| Animal Protocol |
Animal/Disease Models: Female SCID/beige mice were subcutaneously (sc) (sc) implanted with 3×106 Toledo or RS4;11[1].
Doses: 20, 50, 100 mg/kg. Route of Administration: Orally administered daily for 7 days. Experimental Results: Significant antitumor activity was induced in a time- and dose-dependent manner. Animal/Disease Models: SCID/beige female mice bearing RS4;11 tumor xenografts [1]. Doses: 25 and 100 mg/kg. Route of Administration: Single po (oral gavage) treatment. Experimental Results: Concentrations of 25 and 100 mg/kg did not cause platelet loss in vivo. |
| 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.
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| Molecular Formula |
C₄₃H₄₃CLN₄O₆
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|---|---|
| Molecular Weight |
747.277730226517
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| CAS # |
1448525-91-4
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| Related CAS # |
S55746;1448584-12-0
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| 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
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| InChi Key |
RAUZIGXCAJHBEL-WAQYZQTGSA-N
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| InChi Code |
InChI=1S/C43H42N4O6.ClH/c48-34-15-13-32(14-16-34)47(31-10-2-1-3-11-31)43(50)37-23-39(45-17-7-6-12-38(37)45)35-24-40-41(53-28-52-40)25-36(35)42(49)46-26-30-9-5-4-8-29(30)22-33(46)27-44-18-20-51-21-19-44/h1-5,8-11,13-16,23-25,33,48H,6-7,12,17-22,26-28H21H/t33-/m0./s1
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| Chemical Name |
(S)-N-(4-hydroxyphenyl)-3-(6-(3-(morpholinomethyl)-1,2,3,4-tetrahydroisoquinoline-2-carbonyl)benzo[d][1,3]dioxol-5-yl)-N-phenyl-5,6,7,8-tetrahydroindolizine-1-carboxamide
hydrochloride
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| Synonyms |
S55746 hydrochloride S 55746 hydrochloride S-55746
hydrochloride BLC201 hydrochloride BLC 201 hydrochloride BLC-201
hydrochloride
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~200 mg/mL (~267.64 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5 mg/mL (6.69 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 5 mg/mL (6.69 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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