1A-116|cas:1430208-73-3|西域试剂

1A-116,99.79%

产品编号：Bellancom-104064| CAS NO：1430208-73-3| 分子式：C₁₆H₁₆F₃N₃| 分子量：307.31

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货号	价格	库存与货期
Bellancom-104064	￥1800.00	杭州北京（现货）
Bellancom-104064	￥2900.00	杭州北京（现货）
Bellancom-104064	￥5800.00	杭州北京（现货）
Bellancom-104064	￥9400.00	杭州北京（现货）
Bellancom-104064	￥15000.00	杭州北京（现货）

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1A-116

产品介绍

1A-116 是一种对 W56 残基具有特异性的 Rac1 抑制剂，能有效防止 EGF 诱导的 Rac1 激活，并阻断 Rac1-P-Rex1 的相互作用。1A-116 能以昼夜节律依赖的方式诱导细胞凋亡并抑制细胞的增殖、迁移和周期进展。1A-116 在体内也具有较高的抗癌细胞转移活性。

生物活性

1A-116, a potent Rac1 inhibitor, is specific for W56 residues, can prevent EGF-induced Rac1 activation and block Rac1-P-Rex1 interaction. 1A-116 can induce apoptosis and inhibit cell proliferation, migration and cycle progression in a concentration-dependent manner. 1A-116 also demonstrates a high antimetastatic activity in vivo.

体外研究

1A-116 (48 h) inhibits F3II and MDA-MB-231 cells proliferation in a concentration-dependent manner with IC₅₀s of 4 µM and 21 µM, respectively.
1A-116 (1, 10 µM; 12 h) dramatically impaires Rac1 activation, and reduces Rac1-GTP intracellular levels in a concentration-dependent manner in F3II cells.
1A-116 (50, 100 µM; 12 h) blocks Rac1-P-Rex1 interaction.
1A-116 (20 µM; 5 h intervals over 25 h) inhibits LN229 cells proliferation in a circadian manner.
1A-116 (10 µM; 16 h) significantly reduces cell migration at 10 HPS which exhibits temporal dependence. (HPS: After the serum shock, the elapsed time (in hours) is recorded as the hours post-synchronization (HPS)).
1A-116 (20, 50 µM; 6 h) induces cells apoptosis and in a circadian-dependent manner.
1A-116 (100 nM) decreases the thickness of the epidermal layers of Vav2 and Rac1-mediated hyperplasia, but not the PAK1-mediated one, which exhibits the activity of inhibiting Rac1 at the GEF-Rac1 level.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay

Cell Line:	MDA-MB-231, F3II, LN229 cells
Concentration:	20 µM
Incubation Time:	48 h; 5 h intervals over 25 h.
Result:	Inhibited cell proliferation in a concentration-dependent and circadian manner.

Cell Viability Assay

Cell Line:	Ker-CT human keratinocytes cells with oncogenic Vav2/Rac1 F28L/PAK1 Tyrosine 423
Concentration:	100 nM
Incubation Time:
Result:	Inhibited Rac1 activity at the GEF-Rac1 level.

Cell Migration Assay

Cell Line:	LN229 cells
Concentration:	10 µM
Incubation Time:	16 h
Result:	Reduced cell migration at 10 HPS which exhibited temporal dependence.

Apoptosis Analysis

Cell Line:	LN229 cells
Concentration:	20, 50 µM
Incubation Time:	6 h
Result:	Induced cells apoptosis and in a circadian-dependent manner.

Western Blot Analysis

Cell Line:	F3II cells
Concentration:	1, 10 µM
Incubation Time:	12 h
Result:	Blocked Rac1-P-Rex1 interaction. Reduced Rac1-GTP intracellular levels in a concentration-dependent manner.

体内研究
(In Vivo)

1A-116 (3 mg/kg; i.v.; once a day for 21 days) demonstrates a high antimetastatic activity with about 60% formation reduction of total metastatic lung colonies in vivo and shows no apparent toxicity.
1A-116 (20 mg/kg; i.p.; once a day, 73 days for ZT12, 68 days for ZT3) increases survival time when treated at ZT12 compare to ZT3 in tumor-bearing mice. (ZT: Zeitgeber time 12 (ZT12) defined as the time of lights off (local time 7 p.m.) and ZT0 defined as lights on (local time 7 a.m.)).
1A-116 shows good oral availability.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female BALB/c inbred mice (8 to 10-week-old; average 20 g)
Dosage:	3 mg/kg
Administration:	Intravenous injection; once a day for 21 days.
Result:	Demonstrated a high antimetastatic activity.

Animal Model:	Male NIH Swiss foxN1(∆/∆) nude mice (2-month-old; GBM model).
Dosage:	20 mg/kg
Administration:	Intraperitoneal injection (at ZT3, ZT12); once a day, 73 days for ZT12, 68 days for ZT3.
Result:	Increased survival time when treated at ZT12 compared to ZT3 in tumor-bearing mice.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female BALB/c inbred mice (8 to 10-week-old; average 20 g)
Dosage:	3 mg/kg
Administration:	Intravenous injection; once a day for 21 days.
Result:	Demonstrated a high antimetastatic activity.

Animal Model:	Male NIH Swiss foxN1(∆/∆) nude mice (2-month-old; GBM model).
Dosage:	20 mg/kg
Administration:	Intraperitoneal injection (at ZT3, ZT12); once a day, 73 days for ZT12, 68 days for ZT3.
Result:	Increased survival time when treated at ZT12 compared to ZT3 in tumor-bearing mice.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female BALB/c inbred mice (8 to 10-week-old; average 20 g)
Dosage:	3 mg/kg
Administration:	Intravenous injection; once a day for 21 days.
Result:	Demonstrated a high antimetastatic activity.

Animal Model:	Male NIH Swiss foxN1(∆/∆) nude mice (2-month-old; GBM model).
Dosage:	20 mg/kg
Administration:	Intraperitoneal injection (at ZT3, ZT12); once a day, 73 days for ZT12, 68 days for ZT3.
Result:	Increased survival time when treated at ZT12 compared to ZT3 in tumor-bearing mice.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (325.40 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.2540 mL	16.2702 mL	32.5404 mL
5 mM	0.6508 mL	3.2540 mL	6.5081 mL
10 mM	0.3254 mL	1.6270 mL	3.2540 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (8.14 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (8.14 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: 2.5 mg/mL (8.14 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (8.14 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (8.14 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (8.14 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。