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关于此项目
经验公式(希尔记法):
C14H12Cl4N4NaRu
化学文摘社编号:
分子量:
502.14
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
InChI
1S/2C7H6N2.4ClH.Na.Ru/c2*1-2-4-7-6(3-1)5-8-9-7;;;;;;/h2*1-5H,(H,8,9);4*1H;;/q;;;;;;+1;+3/p-4
SMILES string
Cl[Ru-](Cl)(Cl)Cl.C1(C=CC=C2)=C2NN=C1.C3(C=CC=C4)=C4NN=C3.[Na+]
InChI key
WVVOCRYXBTVDRN-UHFFFAOYSA-J
assay
≥98% (elemental analysis)
form
powder
color
, white to very dark grey
solubility
H2O: 2 mg/mL, clear (Warmed)
storage temp.
-10 to -25°C
Quality Level
Biochem/physiol Actions
KP1339 (KP1019 sodium) is a ruthenium-indazole complex-based anticancer agent that induces pronounced apoptosis in sensetive cancer cells (Capan1/HCT116/SW480/KB-3-1 IC50 by MTT assay = 44/50/145/170 µM) via ER homeostasis disruption and caspase 8 activation due to depletion of key cellular chaperones, including BiP/GRP78/HSPA5, in combination with enhanced protein damage. When administered in vivo, KP1339 exhibits anti-tumor efficacy in the murine SA-1 fibrosarcoma model (10.5, 21.0, 42.0 mg/150 µL/kg i.v.).
Ruthenium-indazole complex-based anticancer agent in cultures and in vivo via ER homeostasis disruption by depleting chaperones, including BiP/GRP78/HSPA5.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
法规信息
新产品
此项目有
Interaction with Ribosomal Proteins Accompanies Stress Induction of the Anticancer Metallodrug BOLD-100/KP1339 in the Endoplasmic Reticulum
Angewandte Chemie (International ed. in English), 60, 5063-5068 (2021)
The influence of electroporation on cytotoxicity of anticancer ruthenium(III) complex KP1339 in vitro and in vivo
Anticancer Research, 30, 2055-2063 (2010)
Sensitivity towards the GRP78 inhibitor KP1339/IT-139 is characterized by apoptosis induction via caspase 8 upon disruption of ER homeostasis
Cancer Letters, 404, 79-88 (2017)
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