TL4-12

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

TL4-12 是一种选择性 MAP4K2/GCK 抑制剂，下调 IKZF1 和 BCL-6，并抑制 MM 细胞增殖 (IC50=37 nM) 并诱导细胞凋亡。TL4-12 可用于克服多发性骨髓瘤 (MM) 中免疫调节剂的耐药性。

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 agent resistance in multiple myeloma (MM).

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.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.TL4-12 dose-dependently increases Annexin-V positive cell from 6% (dimethyl sulfoxide) to 13% (1 μM) and 22% (3 μM), respectively.TL4-12 induces apoptosis and cell-cycle arrest in the G0/G1 phase in MM.1S, RPMI-8226, RPMI-8226 cells.

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Others

Other Targets

Immunology/Inflammation related | BCL | Apoptosis

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1620820-12-3

500.52

C25H27F3N6O2

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 8.33 mg/mL (16.64 mM; 超声助溶 (<60°C)

O=C(NC=1C=C(C=C(C1)C(F)(F)F)N2CCN(C)CC2)C3=CC=C(C(OC4=NC=NC(=C4)NC)=C3)C

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(-20℃)

With Ice Pack

≥ 2 years