T-3775440 HCl
This product is for research use only, not for human use. We do not sell to patients.
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| Size | Price | Stock |
|---|---|---|
| 100mg | $2475 | To Be Confirmed |
| 200mg | $3710 | To Be Confirmed |
| 500mg | $6260 | To Be Confirmed |
: Cat #: V5227 CAS #: 1422535-52-1 Purity ≥ 98%
Description: T-3775440 (T3775440) HCl is a novel, potent, selective, and irreversible lysine-specific histone demethylase (LSD1) inhibitor with anticancer activity.
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| Molecular Weight (MW) | 346.85 |
|---|---|
| Molecular Formula | C18H23ClN4O |
| CAS No. | 1422535-52-1 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| SMILES Code | O=C(C1=CN(C)N=C1)NC2=CC=C([C@H]3[C@H](NCC4CC4)C3)C=C2.[H]Cl |
| Synonyms | T 3775440 Hydrochloride; T3775440 Hydrochloride; T-3775440 HCl; T 3775440 HCl; T3775440 HCl; T-3775440 Hydrochloride; |
| Protocol | In Vitro | T-3775440 demonstrates irreversible inhibition of recombinant human LSD1, with a kinact/KI value of 1.7×105 (sec−1 M−1). T-3775440 is highly selective for LSD1 relative to other monoamine oxidases (e.g., MAO-A and MAO-B), with an IC50 value of 2.1 nM). T-3775440 blocks the proliferation of several cell lines as quickly as day 3 of treatment. Notably, the granulocyte/macrophage markers CD86 and CD11b are commonly upregulated on both TF-1a and HEL92.1.7 cells in response to T-3775440 treatment, whereas the erythroid markers CD235a and CD71 are downregulated by this treatment. 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 Vivo | T-3775440 upregulates CD86 mRNA expression in tumor xenografts of HEL92.1.7 cells in a dose-dependent manner following the oral administration of single doses ranging from 3 to 30 mg/kg. To investigate target engagement of this compound in tumors, PI16 expression levels is tested as a direct biomarker. As expected, PI16 suppression is dramatically reversed by T-3775440 treatment. 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. It is found that in mice, T-3775440 treatment results in a transient reduction in platelets, followed by a significant rebound; this is considered a mechanism-based adverse effect of LSD1 inhibition. On a dosing schedule comprising 5 days on/2 days off, a statistically significant difference in body weight is observed between vehicle- and T-3775440–treated tumor xenograft model mice at higher doses. However, efficacious T-3775440 doses are tolerated in all subcutaneous tumor xenograft models. |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 2.8831 mL | 14.4155 mL | 28.8309 mL | 57.6618 mL |
| 5mM | 0.5766 mL | 2.8831 mL | 5.7662 mL | 11.5324 mL |
| 10mM | 0.2883 mL | 1.4415 mL | 2.8831 mL | 5.7662 mL |
| 20mM | 0.1442 mL | 0.7208 mL | 1.4415 mL | 2.8831 mL |
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