TW-37;CS-299;TW37;TW 37;TW-37 USP/EP/BP;TW-37/Bcl-2Inhibitor;TW-37, 10 mM in DMSO;inhibit,Bcl-2 Family,TW37,TW-37,Inhibitor;5-(2-isopropylbenzyl)-N-(4-(2-tert-butylphenylsulfonyl)phenyl)-2,3,4-trihydroxybenzamide;N-[4-(2-tert-Butylphenylsulfonyl)phenyl]-2,3,4-trihydroxy-5-(2-isopropylbenzyl)benzamide;TW-37/N-[4-(2-tert-Butylphenylsulfonyl)phenyl]-2,3,4-trihydroxy-5-(2-isopropylbenzyl)benzamide
insoluble in H2O; ≥19.75 mg/mL in DMSO; ≥3.41 mg/mL in EtOH with gentle warming and ultrasonic
??? ??
??? ??
?? ?? (pKa)
7.86±0.50(Predicted)
??
White to off-white
??
?? ? ?? ??
?? ? ???? ?? (GHS)
????(GHS):
?? ?:
Warning
??·?? ??:
??
??·?? ??
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??
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P- ??
H302
??? ???
?? ?? ?? - ??
?? 4
??
P264, P270, P301+P312, P330, P501
??????:
P264
?? ??? ?? ??? ????.
P264
?? ??? ?? ??? ????.
P270
? ??? ??? ??? ???, ???? ???? ???.
P301+P312
??? ???? ??? ????(??)? ??? ????.
P330
?? ?????.
P501
...? ??? / ??? ?? ???.
NFPA 704
0
2
0
TW-37 C??? ??, ??, ??
??
TW-37 is an inhibitor of the Bcl-2 family proteins Bcl-2, Mcl-1, and Bcl-xL (Kis = 120, 260, and 1,100 nM, respectively). It induces apoptosis, inhibits migration and capillary sprouting, and blocks the expression of the angiogenic chemokines CXCL1 and CXCL8 in endothelial cells. TW-37 decreases the density of functional human microvessels in the severe combined immunodeficient mouse model of human angiogenesis when administered intravenously. It has apoptotic action against leukemia, lymphoma, and pancreatic cancer cells.
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TW-37 is a novel nonpeptide inhibitor to recombinant Bcl-2, Bcl-xL and Mcl-1 with Ki of 0.29 μM, 1.11 μM and 0.26 μM, respectively.
