SML2154
Deltarasin trihydrochloride
≥98% (HPLC)
别名:
(S)-1-Benzyl-2-(4-(2-(2-phenyl-1H-benzo[d]imidazol-1-yl)-2-(piperidin-4-yl)ethoxy)phenyl)-1H-benzo[d]imidazole trihydrochloride, 2-[4-[(2S)-2-(2-Phenyl-1H-benzimidazol-1-yl)-2-(4-piperidinyl)ethoxy]phenyl]-1-(phenylmethyl)-1H-benzimidazole trihydrochloride
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About This Item
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化驗
≥98% (HPLC)
形狀
powder
儲存條件
desiccated
顏色
white to beige
溶解度
H2O: 2 mg/mL, clear
儲存溫度
2-8°C
InChI
1S/C40H37N5O/c1-3-11-29(12-4-1)27-44-36-17-9-7-15-34(36)42-39(44)32-19-21-33(22-20-32)46-28-38(30-23-25-41-26-24-30)45-37-18-10-8-16-35(37)43-40(45)31-13-5-2-6-14-31/h1-22,30,38,41H,23-28H2/t38-/m1/s1
InChI 密鑰
LTZKEDSUXKTTTC-KXQOOQHDSA-N
生化／生理作用
Deltarasin is a membrane-permeable benzimidazole derivative that effectively abolishes cellular KRas plasma membrane localization (5 μM for 1 hr) by blocking KRas-PDEδ interaction via high affinity interaction with PDEδ prenyl-binding pocket (KD = 38 nM). Deltarasin inhibits oncogenic KRas-dependent proliferation (by ~50% of Panc-Tu-I cells; 5μM for 70 hrs) and survival (52% and 46% death induction of Panc-Tu-I and Capan-1 cells, respectively; 5μM for 24 hrs) in human pancreatic ductal adenocarcinoma (PDAC) cultures and is efficacious against Panc-Tu-I xenograft-derived tumor growth in mice in vivo (60% and 80% retardation on day 9, respectively, with 15 mg/kg q.d. or 10 mg/kg b.i.d. via i.p.).
儲存類別代碼
11 - Combustible Solids
水污染物質分類（WGK）
WGK 3
Sandip Murarka et al.
Chemistry (Weinheim an der Bergstrasse, Germany), 23(25), 6083-6093 (2016-11-04)
The K-Ras GTPase is a major target in anticancer drug discovery. However, direct interference with signaling by K-Ras has not led to clinically useful drugs yet. Correct localization and signaling by farnesylated K-Ras is regulated by the prenyl binding protein
Gunther Zimmermann et al.
Journal of medicinal chemistry, 57(12), 5435-5448 (2014-06-03)
K-Ras is one of the most frequently mutated signal transducing human oncogenes. Ras signaling activity requires correct cellular localization of the GTPase. The spatial organization of K-Ras is controlled by the prenyl binding protein PDEδ, which enhances Ras diffusion in
Jianman Guo et al.
American journal of cancer research, 7(4), 923-934 (2017-05-05)
Patients with Neurofibromatosis type 1 (NF1) and Neurofibromatosis type 2 (NF2) are predisposed to tumors of the nervous system. NF1 patients predominantly develop neurofibromas, and Malignant Peripheral Nerve Sheath Tumors (MPNST) while NF2 patients develop schwannomas and meningiomas. Here we
Philipp Küchler et al.
Bioorganic & medicinal chemistry, 26(8), 1426-1434 (2017-09-25)
Prenylation is a post-translational modification that increases the affinity of proteins for membranes and mediates protein-protein interactions. The retinal rod rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit delta (PDEδ) is a prenyl binding protein that is essential for the shuttling of small
Malte Schmick et al.
Cell, 157(2), 459-471 (2014-04-15)
KRas is a major proto-oncogene product whose signaling activity depends on its level of enrichment on the plasma membrane (PM). This PM localization relies on posttranslational prenylation for membrane affinity, while PM specificity has been attributed to electrostatic interactions between
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