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SML3695

Sabutoclax

≥98% (HPLC)

别名:

(1R)-1,1′,6,6′,7,7′-Hexahydroxy-3,3′-dimethyl-N5,N5′-bis[(2R)-2-phenylpropyl]-[2,2′-binaphthalene]-5,5′-dicarboxamide, (RS)-1,1′,6,6′,7,7′-Hexahydroxy-3,3′-dimethyl-N5-((R)-2-phenylpropyl)-N5′-((R)-2-phenylpropyl)-2,2′-binaphthyl-5,5′-dicarboxamide, BI-97C1, BI97C1

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关于此项目

经验公式（希尔记法）:
C42H40N2O8
化学文摘社编号:
1354327-17-5
分子量:
700.78
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
MFCD26142645
Assay:
≥98% (HPLC)
Form:
powder
Quality level:
100
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Quality Level

100

assay

≥98% (HPLC)

form

powder

color

white to beige

shipped in

wet ice

storage temp.

-10 to -25°C

SMILES string

O=C(C1=C(O)C(O)=CC2=C(O)C(C3=C(C)C=C4C(C(NC[C@@H](C5=CC=CC=C5)C)=O)=C(O)C(O)=CC4=C3O)=C(C)C=C12)NC[C@@H](C6=CC=CC=C6)C

InChI

1S/C42H40N2O8/c1-21-15-27-29(17-31(45)39(49)35(27)41(51)43-19-23(3)25-11-7-5-8-12-25)37(47)33(21)34-22(2)16-28-30(38(34)48)18-32(46)40(50)36(28)42(52)44-20-24(4)26-13-9-6-10-14-26/h5-18,23-24,45-50H,19-20H2,1-4H3,(H,43,51)(H,44,52)/t23-,24-/m0/s1

InChI key

RAYNZUHYMMLQQA-ZEQRLZLVSA-N

Biochem/physiol Actions

Potent inhibitor against antiapoptotic Bcl-2 family proteins (Bcl-xL, Bcl-2, Mcl-1, Bfl-1) with anti-cancer efficacy in cultures and in vivo.



Sabutoclax (BI-97C1) is a potent inhibitor against antiapoptotic Bcl-2 family proteins (IC50 in nM against BH3 peptide binding = 310/Bcl-xL, 320/Bcl-2, 200/Mcl-1, 620/Bfl-1) that induces apoptosis in cancer cultures (EC50 in nM = 49/BP3, 130/PC3, 420/H460) with little cytotoxicity against bax-/-bak-/- cells. Sabutoclax anti-tumore efficacy in vivo, including a Bcl-2 transgenic model (42 mg/kg i.p. in mice expressing human Bcl-2 in splenic B-cells) and a M2182 prostate cancer xenograft model (1,3, 5 mg/kg q.o.d. i.p. in mice).

pictograms

Exclamation mark
GHS07

signalword

Warning

hcodes

H302

Hazard Classifications

Acute Tox. 4 Oral

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

法规信息

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分析证书(COA)

Lot/Batch Number
0000374886
0000374881
0000374881
0000374886

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Jun Wei et al.
Journal of medicinal chemistry, 53(10), 4166-4176 (2010-05-07)
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Currently, there is no cure for Alzheimer's disease (AD). Therapeutics that can modify the early stage of AD are urgently needed. Recent studies have shown that the pathogenesis of AD is closely regulated by an endo/lysosomal asparaginyl endopeptidase (AEP). Inhibition

全球贸易项目编号

货号GTIN
SML3695-50MG04065269137566
SML3695-10MG04065269137559