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经验公式(希尔记法):
C32H48N4O8 · xHCl
化学文摘社编号:
分子量:
616.75 (free base basis)
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
产品名称
17-DMAG, A potent antitumor analog of 17-AAG that binds to the ATPase site of human Hsp90α with high affinity and displays excellent bioavailability and aqueous solubility.
InChI
1S/C32H48N4O8.ClH/c1-18-14-22-27(34-12-13-36(5)6)24(37)17-23(29(22)39)35-31(40)19(2)10-9-11-25(42-7)30(44-32(33)41)21(4)16-20(3)28(38)26(15-18)43-8;/h9-11,16-18,20,25-26,28,30,34,38H,12-15H2,1-8H3,(H2,33,41)(H,35,40);1H/b11-9-,19-10+,21-16+;/t18-,20+,25+,26+,28-,30+;/m1./s1
InChI key
DFSYBWLNYPEFJK-IHLRWNDRSA-N
assay
≥95% (TLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
protect from light
color
purple
solubility
water: 10 mg/mL
DMSO: 5 mg/mL
shipped in
wet ice
storage temp.
−20°C
Quality Level
Biochem/physiol Actions
主要靶标
17-DMAG
17-DMAG
产物不与ATP竞争。
可逆:否
在NCI 60-细胞面板体外活性筛选中,GI50=51 nM(17-DMAG)和120 nM(17-AAG)
细胞渗透性:否
Disclaimer
毒性:标准处理(A)
General description
17-AAG(目录编号100068)的有效的抗肿瘤类似物,以高亲和力与人Hsp90α的ATPase位点结合(在NCI 60面板体外活性筛选中,GI50=51 nM(17-DMAG)和120 nM(17-AAG)),并显示出出色的生物利用度和水溶性。
17-AAG(目录编号100068)的细胞可渗透性,水溶性,有效的抗肿瘤类似物,以高亲和力与人Hsp90α的ATPase位点结合(在NCI 60-细胞面板体外活性筛选中,GI50=51 nM(17-DMAG)和120 nM(17-AAG))。
Other Notes
Tian, Z.Q., et al. 2004.Bioorg.Med. Chem.12, 5317.
Jez, J.M., et al. 2003.Chem. Biol.10, 361.
Egorin, M.J., et al. 2002.Cancer Chemother.Pharmacol.49, 7.
Jez, J.M., et al. 2003.Chem. Biol.10, 361.
Egorin, M.J., et al. 2002.Cancer Chemother.Pharmacol.49, 7.
Packaging
用惰性气体包装
Preparation Note
在复溶后,分装并冷冻保存(-20°C)。储备溶液在-20°C下可稳定保存至多3个月。
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Behnoush Khaledian et al.
Cancer science, 112(3), 1225-1234 (2020-12-29)
We have previously identified receptor tyrosine kinase-like orphan receptor 1 (ROR1) as a direct transcriptional target of TTF-1/NKX2-1, a lineage-survival oncogene in lung adenocarcinoma. ROR1 sustains prosurvival signaling from multiple receptor tyrosine kinases including epidermal growth factor receptor, MET, and
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