BI-3406; BI 3406; BI3406；compound I-13；CAS#2230836-55-0 DKM中国

BI-3406; BI 3406; BI3406；compound I-13（CAS#2230836-55-0 目录号D808916） KRAS/SOS1抑制剂

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BI-3406 (compound I-13) 是一种有效的、选择性和口服活性的抑制剂，可抑制 KRAS 和 Son of Sevenless 1 (SOS1) 之间的相互作用，其IC50值为5 nM。BI-3406 可减少 GTP-loaded KRAS 的形成，并抑制MAPK信号通路。BI-3406 具有抗肿瘤的活性。

规格	价格	库存
5mg	￥ 3312.00	100
10mg	￥ 6089.00	100
25mg	￥ 9876.00	100

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概述

别名	BI-3406; BI 3406; BI3406；compound I-13
产品名	BI-3406
CAS号	2230836-55-0
目录号	D808916
化学式	C₂₃H₂₅F₃N₄O₃
分子量	462.46
溶解度	Ethanol: 100 mg/mL (216.23 mM); DMSO: 100 mg/mL (216.23 mM)
靶点	SOS1-IN-2 是一种有效的选择性 SOS1 抑制剂，IC50 为 6 nM，详细信息请参考专利文献 WO2018115380A1 中的化合物 I-6。
储存条件	Store at -20°C
用途	仅供科学研究使用!不能用于人体及动物治疗
纯度	>99%

质控及产品安全说明书

Datasheet

详情

生物活性

靶点及简介 ：BI-3406 (compound I-13) 是一种有效的、选择性和口服活性的抑制剂，可抑制 KRAS 和 Son of Sevenless 1 (SOS1) 之间的相互作用，其IC50值为5 nM。BI-3406 可减少 GTP-loaded KRAS 的形成，并抑制MAPK信号通路。BI-3406 具有抗肿瘤的活性。它是一种有效的选择性 SOS1 抑制剂，详细信息请参考专利文献 WO2018115380A1 中的化合物 I-6。

分子量	462.46
化学式	C₂₃H₂₅F₃N₄O₃
CAS号	2230836-55-0
储存条件	3年	-20°C	粉状
储存条件	1年	-80°C	溶于溶剂

体外研究：

BI-3406 is a highly potent and selective, orally bioavailable SOS1::KRAS inhibitor which binds to the catalytic domain of the guanine nucleotide exchange factor (GEF) SOS1 thereby preventing the interaction with KRAS-GDP. BI-3406 does not block the interaction of KRAS with SOS2 but elicits activity on a broad panel of KRAS oncogenic variants, including all major G12 and G13 oncoproteins. In KRAS-dependent cancers, BI-3406 potently reduces the formation of GTP-loaded KRAS, and inhibits MAPK pathway signaling. Down-modulation of this signaling cascade by BI-3406 in KRAS G12 or G13 mutant cells effectively limits cell proliferation.[2]

体内研究:

BI-3406 modulates signaling, as assessed by p-ERK and target genes, and displays marked anti-tumor efficacy in KRAS mutant xenografts. Due to BI-3406 blocking the negative feedback relief induced by MAPK inhibition, it has the potential to sensitize KRASdependent cancers to MEK inhibitor treatment. Combination with MEK inhibition leads to profound pathway blockade and tumor regressions in vivo.[2]

细胞实验：

Cell lines: NCI-H358, A-549 cells, MIA PaCa-2 cells, PC-9 cells

Concentrations: 61.7 nM, 185 nM, 556 nM, 1670 nM, 5000 nM

Incubation Time: 24 h, 48 h, 72 h

Method:

200000 cells are seeded in each well of the 24-well plate. Cells are incubated with the respective concentration of BI-3406 in monotherapy or in combination for 24 h, 48 h and 72 h. At the respective time point complete medium is aspirated and cells are lysed by using 100 mL lysate buffer from a commercially available assay whole lysate kit.[1]

动物实验：

Animal Models: 6-8 weeks female BomTacNMRI-Foxn1 nu mice with Tumor xenografts

Dosages: 10 mg/kg Administration: Oral gavage[1]

验证及参考文献

验证：

参考文献：

溶解度及制备方案
DMSO
92 mg/mL (198.94 mM)
Ethanol
92 mg/mL (198.94 mM)
Water
Insoluble
制备储备液
浓度溶剂体积质量
1 mg
5 mg
10 mg
1 mM
2.1623 mL
10.8117 mL
21.6235 mL
5 mM
0.4325 mL
2.1623 mL
4.3247 mL
10 mM
0.2162 mL
1.0812 mL
2.1623 mL
50 mM
0.0432 mL
0.2162 mL
0.4325 mL

关键词：BI-3406, BI-3406供应商, Ras抑制剂, 购买BI-3406, BI-3406溶解度, BI-3406结构式

DMSO	92 mg/mL (198.94 mM)
Ethanol	92 mg/mL (198.94 mM)
Water	Insoluble

浓度溶剂体积质量	1 mg	5 mg	10 mg
1 mM	2.1623 mL	10.8117 mL	21.6235 mL
5 mM	0.4325 mL	2.1623 mL	4.3247 mL
10 mM	0.2162 mL	1.0812 mL	2.1623 mL
50 mM	0.0432 mL	0.2162 mL	0.4325 mL