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T-3775440 hydrochloride

Cat. No. M9644
T-3775440 hydrochloride Structure
Synonym:

T-3775440 HCl

Size Price Availability
5mg USD 460 4-7 Days
25mg USD 1500 4-7 Days
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

T-3775440 hydrochloride is a potent, selecitve, irreversible LSD1 inhibitor with IC50 value of 2.1 nM. T-3775440 is highly selective for LSD1 relative to other monoamine oxidases (e.g., MAO-A and MAO-B), with IC50 value of 2.1 nM. In CMK11-5 cells, CD86 mRNA expression is also clearly upregulated by T-3775440 in a concentration-dependent manner, although only a modest increase in cell surface CD86 expression is observed. T-3775440 treatment disrupts the LSD1-GFI1B association in a concentration-dependent manner. T-3775440 decreases LSD1 binding but not GFI1B binding and increases the level of dimethylated H3K4 at the PI16 locus. 

In a TF-1a (AEL) tumor xenograft model, T-3775440 exhibits significant antitumor effects, with 15-day T/C values of 15.6% and <0% at doses of 20 and 40 mg/kg, respectively. T-3775440 also exhibits potent antitumor effects in an additional AEL model of HEL 92.1.7 and an AMKL model of CMK11-5, leading to nearly complete tumor growth suppression during the dosing period.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 346.85
Formula C18H23ClN4O
CAS Number 1422535-52-1
Purity >99%
Solubility DMSO ≥ 25 mg/mL
Water ≥ 10 mg/mL
Storage -20°C, dry, protect from light, sealed
References

Synergistic anti-AML effects of the LSD1 inhibitor T-3775440 and the NEDD8-activating enzyme inhibitor pevonedistat via transdifferentiation and DNA rereplication
Y Ishikawa, et al. Oncogenesis. 2017 Sep 11;6(9):e377. PMID: 28892104.

A Novel LSD1 Inhibitor T-3775440 Disrupts GFI1B-Containing Complex Leading to Transdifferentiation and Impaired Growth of AML Cells
Yoshinori Ishikawa, et al. Mol Cancer Ther. 2017 Feb;16(2):273-284. PMID: 27903753.

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  Catalog
Abmole Inhibitor Catalog 2017




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