T-3775440 hydrochloride
- Product Name
- T-3775440 hydrochloride
- CAS No.
- 1422535-52-1
- Chemical Name
- T-3775440 hydrochloride
- Synonyms
- T-3775440HCl;T 3775440;T3775440;T-3775440 hydrochloride;T-3775440 hydrochloride, 10 mM in DMSO;N-(4-(trans-2-((Cyclopropylmethyl)amino)cyclopropyl)phenyl)-1-methyl-1H-pyrazole-4-carboxamide hydrochloride;T3775440 hydrochloride,T-3775440,inhibit,T3775440,T 3775440,Inhibitor,T 3775440 hydrochloride,Histone Demethylase
- CBNumber
- CB24668572
- Molecular Formula
- C18H23ClN4O
- Formula Weight
- 346.86
- MOL File
- 1422535-52-1.mol
T-3775440 hydrochloride Property
- storage temp.
- Store at -20°C
- solubility
- DMSO : ≥ 30.18 mg/mL (87.01 mM)
- form
- Solid
- color
- Light yellow to yellow
- InChI
- InChI=1/C18H22N4O.ClH/c1-22-11-14(10-20-22)18(23)21-15-6-4-13(5-7-15)16-8-17(16)19-9-12-2-3-12;/h4-7,10-12,16-17,19H,2-3,8-9H2,1H3,(H,21,23);1H/t16-,17+;/s3
- InChIKey
- XYFPAGOQZFSLFH-NAHYZYKJNA-N
- SMILES
- N([C@@H]1C[C@H]1C1C=CC(NC(C2C=NN(C)C=2)=O)=CC=1)CC1CC1.Cl |&1:1,3,r|
N-Bromosuccinimide Price
- Product number
- BT168491
- Product name
- T 3775440 hydrochloride
- Packaging
- 5mg
- Price
- $300
- Updated
- 2021/12/16
- Product number
- CS-0023825
- Product name
- T-3775440hydrochloride
- Purity
- 99.13%
- Packaging
- 5mg
- Price
- $450
- Updated
- 2021/12/16
- Product number
- 7208EA
- Product name
- T-3775440Hydrochloride
- Packaging
- 5mg
- Price
- $455
- Updated
- 2021/12/16
- Product number
- CS-0023825
- Product name
- T-3775440hydrochloride
- Purity
- 99.13%
- Packaging
- 10mg
- Price
- $750
- Updated
- 2021/12/16
- Product number
- BT168491
- Product name
- T 3775440 hydrochloride
- Packaging
- 25mg
- Price
- $905
- Updated
- 2021/12/16
T-3775440 hydrochloride Chemical Properties,Usage,Production
Uses
T-3775440 (hydrochloride) is an irreversible lysine-specific histone demethylase (LSD1) inhibitor with an IC50 value of 2.1 nM.
Biological Activity
| Target | Value |
| LSD1 () | 2.1 nM |
Biological Activity
T-3775440 hydrochloride is an irreversible LSD1 inhibitor. It is highly selective for LSD1 relative to other monoamine oxidases with IC50 of 2.1 nM.
in vitro
T-3775440 hydrochloride enhances the transdifferentiation of erythrocytes/megakaryocytes to granule-like monocytes. It disrupts the interaction of LSD1 and GFI1B. AEL (TF-1a, HEL92.1.7) cells and AMKL (CMK11-5, M07e) cells were treated with T-3775440 for 48 hours, which induced cell cycle arrest and apoptosis. In TF-1a and CMK11-5 cells, treatment with T-3775440 increased cells in G1 and sub-G1 phases.
in vivo
T-3775440 inhibits tumor growth in a mouse xenograft model of AML. In mice T-3775440 hydrochloride caused a transient decrease in platelets followed by a large rebound. After a single dose, it had no apparent effect on red blood cell counts. T-3775440 hydrochloride also exerted antitumor activity in AEL (HEL 92.1.7) model and AMKL (CMK11-5) model.
IC 50
KDM1/LSD1
References
[1] Ishikawa Y, et al. A Novel LSD1 Inhibitor T-3775440 Disrupts GFI1B-Containing Complex Leading to Transdifferentiation and Impaired Growth of AML Cells. Mol Cancer Ther. 2017 Feb;16(2):273-284. DOI:10.1158/1535-7163.MCT-16-0471
T-3775440 hydrochloride Preparation Products And Raw materials
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