TL4-12

Modify Date: 2024-01-16 20:43:20

TL4-12 Structure
TL4-12 structure
Common Name TL4-12
CAS Number 1620820-12-3 Molecular Weight 500.516
Density 1.3±0.1 g/cm3 Boiling Point 586.8±50.0 °C at 760 mmHg
Molecular Formula C25H27F3N6O2 Melting Point N/A
MSDS N/A Flash Point 308.7±30.1 °C

 Use of TL4-12


TL4-12 is a selective MAP4K2/GCK inhibitor, dose-dependently downregulates IKZF1 and BCL-6 and leads to MM cell proliferation inhibition (IC50=37 nM) accompanied by induction of apoptosis. TL4-12 can be used to overcome immunomodulatory drug resistance in multiple myeloma (MM)[1].

 Names

Name 4-Methyl-3-{[6-(methylamino)-4-pyrimidinyl]oxy}-N-[3-(4-methyl-1-piperazinyl)-5-(trifluoromethyl)phenyl]benzamide
Synonym More Synonyms

 TL4-12 Biological Activity

Description TL4-12 is a selective MAP4K2/GCK inhibitor, dose-dependently downregulates IKZF1 and BCL-6 and leads to MM cell proliferation inhibition (IC50=37 nM) accompanied by induction of apoptosis. TL4-12 can be used to overcome immunomodulatory drug resistance in multiple myeloma (MM)[1].
Related Catalog
In Vitro TL4 12 (0-5 µM; 4 days) shows antiproliferation activity with an IC50 value of 37 nM for MM cells, and with IC50s of 1.62, 3.7, 4.4, 5.7, 10, 32, 49, 19 µM for JJN3, MM1.S, H929, RPMI-8226, MOLP-8, SKMM2, LP-1, U266 cells, respectively[1]. .TL4-12 (0, 1, 3 µM; 24 h) dose-dependently decreases IKZF1, c-MYC, and BCL-6 protein expression and increases p53 level in K-RASG12A MM.1S cells[1]. TL4-12 dose-dependently increases Annexin-V positive cell from 6% (dimethyl sulfoxide) to 13% (1 μM) and 22% (3 μM), respectively[1]. TL4-12 induces apoptosis and cell-cycle arrest in the G0/G1 phase in MM.1S, RPMI-8226, RPMI-8226 cells[1].
References

[1]. Shirong Li, et al. Targeting the GCK pathway: a novel and selective therapeutic strategy against RAS-mutated multiple myeloma. Blood. 2021 Apr 1;137(13):1754-1764.

 Chemical & Physical Properties

Density 1.3±0.1 g/cm3
Boiling Point 586.8±50.0 °C at 760 mmHg
Molecular Formula C25H27F3N6O2
Molecular Weight 500.516
Flash Point 308.7±30.1 °C
Exact Mass 500.214752
LogP 6.58
Vapour Pressure 0.0±1.6 mmHg at 25°C
Index of Refraction 1.612

 Synonyms

4-Methyl-3-{[6-(methylamino)-4-pyrimidinyl]oxy}-N-[3-(4-methyl-1-piperazinyl)-5-(trifluoromethyl)phenyl]benzamide
Benzamide, 4-methyl-3-[[6-(methylamino)-4-pyrimidinyl]oxy]-N-[3-(4-methyl-1-piperazinyl)-5-(trifluoromethyl)phenyl]-
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