Description
S2157, a N-alkylated tranylcypromine (TCP) derivative, is a potent lysine-specific demethylase 1 (LSD1) inhibitor. S2157 increases H3K9 methylation and reciprocal H3K27 deacetylation at super-enhancer regions. S2157 induces apoptosis in TCP-resistant T-cell acute lymphoblastic leukemia (T-ALL) cells by repressing transcription of the NOTCH3 and TAL1 genes. S2157 efficiently pass through the blood-brain barrier and can almost completely eradicate CNS leukemia in mice transplanted with T-ALL cells.
Product information
CAS Number: 2262488-39-9
Molecular Weight: 451.94
Formula: C23H28ClF2N3O2
Chemical Name: 2-{[(1R,2S)-2-[2-(benzyloxy)-3,5-difluorophenyl]cyclopropyl]amino}-1-(4-methylpiperazin-1-yl)ethan-1-one hydrochloride
Smiles: Cl.CN1CCN(CC1)C(=O)CN[C@@H]1C[C@H]1C1=CC(F)=CC(F)=C1OCC1C=CC=CC=1 |&1:12,14|
InChiKey: PUXYOFXCUCMFSQ-OZYANKIXSA-N
InChi: InChI=1S/C23H27F2N3O2.ClH/c1-27-7-9-28(10-8-27)22(29)14-26-21-13-18(21)19-11-17(24)12-20(25)23(19)30-15-16-5-3-2-4-6-16;/h2-6,11-12,18,21,26H,7-10,13-15H2,1H3;1H/t18-,21+;/m0./s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
S2157 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. S2157 (4-20 µM; 72 hours) modestly inhibits mitogen-activated normal T-lymphocytes. S2157 (4-8 µM; 24 hours) induces apoptosis and down-regulates the expression of NOTCH3 and TAL1 proteins in T-cell acute lymphoblastic leukemia (T-ALL) cells.
In Vivo:
S2157 (50 mg/kg; IP; 3 times a week; for 28 days) causes the size of subcutaneous tumors reduced to less than 20% of that in the untreated control. S2157 (50 mg/kg; IP) has a T1/2 of 0.88 hours, a Cmax of 4.33 μM and an AUC of 5.75 μM•h. S2157 (30 mg/kg or 50 mg/kg; twice a week for 3 weeks) almost completely suppressed the growth of MOLT4 cells in most but not all NOD/SCID mice with MOLT4 cells. S2157 eradicates CNS leukemia in murine xenotransplanted models.
Products are for research use only. Not for human use.
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