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经验公式(希尔记法):
C22H30O2S
化学文摘社编号:
分子量:
358.54
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
MDL number:
产品名称
Salirasib, ≥98% (HPLC)
InChI
1S/C22H30O2S/c1-17(2)9-7-10-18(3)11-8-12-19(4)15-16-25-21-14-6-5-13-20(21)22(23)24/h5-6,9,11,13-15H,7-8,10,12,16H2,1-4H3,(H,23,24)/b18-11+,19-15+
SMILES string
O=C(O)C1=CC=CC=C1SC/C=C(C)/CC/C=C(C)/CCC=C(C)C
InChI key
WUILNKCFCLNXOK-CFBAGHHKSA-N
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 20 mg/mL, clear
storage temp.
−20°C
Quality Level
相关类别
Application
Salirasib已被用作法呢基转移酶抑制剂。
Biochem/physiol Actions
Salirasib(S-反式,反式-法呢基硫代水杨酸/FTS)是一种能够阻断所有形式的Ras的合成小分子,它不同于因可替代的膜结合机制而无法对K-Ras和N-Ras功能进行抑制的法尼基转移酶抑制剂。Salirasib与吉西他滨一起在转移性胰腺腺癌(PDA)的临床前模型中表现出了抗肿瘤活性和生物标志物调节作用。 它也被用作肺癌的一种有效疗法。
Salirasib(法呢基硫代水杨酸)是一种RAS抑制剂。
Salirasib(法呢基硫代水杨酸)是一种RAS抑制剂,可通过从膜上去除法呢基化蛋白而促进Ras降解。 Salirasib在体外和体内模型中会损害下游信号转导并对正在增殖肿瘤细胞的生长和迁移进行抑制。 Salirasib(法呢基硫代水杨酸)最近被证明具有显著的抗炎症和抗关节炎特性。
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
A phase II trial of Salirasib in patients with lung adenocarcinomas with KRAS mutations.
Riely G J, et al.
Journal of Thoracic Oncology : Official Publication of the International Association for the Study of Lung Cancer, 6(8), 1435-1437 (2011)
Suppression of lung cancer tumor growth in a nude mouse model by the Ras inhibitor salirasib (farnesylthiosalicylic acid).
Zundelevich A, et al.
Molecular Cancer Therapeutics, 6(6), 1765-1773 (2007)
Nofar Erlichman et al.
Cancers, 14(4) (2022-02-26)
Therapies targeting the PD-L1/PD-1 axis have recently been introduced to triple-negative breast cancer (TNBC) with limited efficacy, suggesting that this axis promotes tumor progression through mechanisms other than immune suppression. Here, we over-expressed WT-PD-L1 in human TNBC cells (express endogenous
Membrane localization of acetylated CNK1 mediates a positive feedback on RAF/ERK signaling.
Fischer A, et al.
Science Advances, 3(8), e1700475-e1700475 (2017)
Orally administered FTS (salirasib) inhibits human pancreatic tumor growth in nude mice.
Haklai R, et al.
Cancer Chemotherapy and Pharmacology, 61(1), 89-96 (2008)
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