TAK-243

Research use only, not for human use.

TAK-243 (MLN-7243, AOB87172) is a small-molecule, cell-permeable inhibitor of ubiquitin-activating enzyme E1 (UAE1).

TAK-243 (MLN-7243, AOB87172) is a small-molecule, cell-permeable inhibitor of ubiquitin-activating enzyme E1 (UAE1); blocks ssential monoubiquitination events within the translesion synthesis, and homologous recombination (HR) pathways; shows synergistic and additive anti-tumor combination benefits in vivo combined with carboplatin and docetaxel.Solid Tumors Phase 1 Clinical(In Vitro):TAK-243 shows anti-proliferative effect on a panel of cell lines derived from hematologic and solid tumors with variable EC50 values that ranged from 0.006 μM to 1.31 μM.TAK-243 reduces growth and viability of human AML cell lines (OCI-AML2, TEX, U937 and NB4) in a concentration- and time-dependent manner with IC50s ranging from 15-40 nM after treatment for 48 hours.(In Vivo):TAK-243 significantly delays tumor growth in mice (T/C=0.02) with no toxicity as evidenced by no changes in mouse body weight, serum chemistry, or organ histology. TAK-243 reduces primary AML tumor burden in both tested samples without toxicity.

——

——

MLN7243 | MLN-7243 | AOB87172 | AOB-87172

Proteasome/Ubiquitin

E1

E1

Cancer

Solid Tumors

1450833-55-2

519.514

C19H20F3N5O5S2

>98% (HPLC)

DMSO : 50 mg/mL 96.24 mM; H2O : 1 mg/mL1.92 mM

COS(=O)(=O)N[C@H]1C[C@H]([C@@H]([C@@H]1O)O)NC2=CC=NC3=CC(=NN23)C4=CC(=CC=C4)SC(F)(F)F

Methyl ((1S,2R,3S,4R)-2,3-dihydroxy-4-((2-(3-((trifluoromethyl)thio)phenyl)pyrazolo[1,5-a]pyrimidin-7-yl)amino)cyclopentyl)sulfamate

(-20℃)

With Ice Pack

≥ 2 years