S2116
Based on 1 Customer Validation
S2116, a N-alkylated tranylcypromine (TCP) derivative, is a potent lysine-specific demethylase 1 (LSD1) inhibitor. S2116 increases H3K9 methylation and reciprocal H3K27 deacetylation at super-enhancer regions. S2116 induces apoptosis in TCP-resistant T-cell acute lymphoblastic leukemia (T-ALL) cells by repressing transcription of the NOTCH3 and TAL1 genes. S2116 significantly retardes the growth of T-ALL cells in xenotransplanted mice.
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- Purity : 98.05%
- CAS No.: 2262489-89-2
- 화학식: C22H26ClF2N3O2
- 분자량:437.91
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- Protocol
- 순도&문서
- References
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Help & FAQs
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Biological Activity
제품 설명
IC50 & Target
LSD1[1]
In Vitro
S2116 is particularly effective for T-ALL cell lines with the IC50 values between 1.1 µM for human T-ALL cell lines CEM and 6.8 µM for MOLT4[1].
S2116 (4-20 µM; 72 hours) modestly inhibits mitogen-activated normal T-lymphocytes[1].
S2116 (4-8 µM; 24 hours) induces apoptosis and down-regulates the expression of NOTCH3 and TAL1 proteins in T-ALL cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Normal T-lymphocytes
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Concentration:4, 8, 12, 16, 20 µM
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Incubation Time:For 72 hours
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Result:Modestly inhibited mitogen-activated normal T-lymphocytes.
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Cell Line:T-cell acute lymphoblastic leukemia (T-ALL) cells
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Concentration:4, 6, 8 µM
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Incubation Time:For 24 hours
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Result:Induced apoptosis, as evidenced by increased annexin-V reactivity on flow cytometry in T-ALL cells in a dose- and time-dependent manner without affecting cell cycle distribution.
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Cell Line:T-ALL cells
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Concentration:4, 6, 8 µM
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Incubation Time:For 24 hours
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Result:Down-regulated the expression of NOTCH3 and TAL1 proteins in T-ALL cells.
In Vivo
S2116 (50 mg/kg; IP) has a T1/2 of 3.76 hours, a Cmax of 12.7 μM and an AUC of 59.2 μM•h[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Nonobese diabetic/severe combined immunodeficiency (NOD/SCID) mice with MOLT4 cells[1]
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Dosage:50 mg/kg
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Administration:IP; 3 times a week; for 28 days
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Result:The size of subcutaneous tumors reduced to less than 20% of that in the untreated control.
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Animal Model:8-week-old ICR mice[1]
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Dosage:50 mg/kg (Pharmacokinetic Analysis)
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Administration:IP
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Result:Had a T1/2 of 3.76 hours, a Cmax of 12.7 μM and an AUC of 59.2 μM•h.
Chemical Information
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CAS No. 2262489-89-2
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Appearance Solid
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분자량 437.91
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화학식 C22H26ClF2N3O2
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Color Off-white to light yellow
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SMILES
FC1=CC(F)=C(OCC2=CC=CC=C2)C([C@H]3[C@H](NCC(N4C[C@@H](N)CC4)=O)C3)=C1.[H]Cl
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
용액&용해도
In Vitro:
DMSO : 100 mg/mL (228.36 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
순도&문서
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Data Sheet (277 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2836 mL | 11.4179 mL | 22.8357 mL | 57.0894 mL |
| 5 mM | 0.4567 mL | 2.2836 mL | 4.5671 mL | 11.4179 mL | |
| 10 mM | 0.2284 mL | 1.1418 mL | 2.2836 mL | 5.7089 mL | |
| 15 mM | 0.1522 mL | 0.7612 mL | 1.5224 mL | 3.8060 mL | |
| 20 mM | 0.1142 mL | 0.5709 mL | 1.1418 mL | 2.8545 mL | |
| 25 mM | 0.0913 mL | 0.4567 mL | 0.9134 mL | 2.2836 mL | |
| 30 mM | 0.0761 mL | 0.3806 mL | 0.7612 mL | 1.9030 mL | |
| 40 mM | 0.0571 mL | 0.2854 mL | 0.5709 mL | 1.4272 mL | |
| 50 mM | 0.0457 mL | 0.2284 mL | 0.4567 mL | 1.1418 mL | |
| 60 mM | 0.0381 mL | 0.1903 mL | 0.3806 mL | 0.9515 mL | |
| 80 mM | 0.0285 mL | 0.1427 mL | 0.2854 mL | 0.7136 mL | |
| 100 mM | 0.0228 mL | 0.1142 mL | 0.2284 mL | 0.5709 mL |
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