GlpBio

VY-3-135

目录号: GC64681纯度: >99.00%
VY-3-135是一种强效且具有口服稳定性的ACSS2抑制剂，IC50值为44±3.85nM，水溶性为21.7μM。
VY-3-135
Cas No.: 1824637-41-3
规格价格库存数量操作
1mg¥700.00现货
1
5mg¥1,400.00现货
1
10mg¥2,240.00现货
1
25mg¥3,640.00现货
1
10mM (in 1mL DMSO)¥1,323.00现货
1
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    31, 1291–1307 (2021)

产品描述 Description

VY-3-135 is a potent and orally stable ACSS2 inhibitor with an IC50 value of 44±3.85nM and a water solubility of 21.7μM[1]. VY-3-135 is currently used in anti-breast cancer studies and derivative screening assays[2-3].

In vitro, VY-3-135 treatment at 100μM for 48 hours significantly inhibited the proliferation and cell survival of MDA-MB-231BR cells and 4T1 cells[4].

In vivo, VY-3-135 treatment (100mg/kg) through oral gavage daily for 30 days significantly inhibited tumor growth and obviously improved survival in a mouse model of breast cancer xenografts, resulting in enhanced immune cell infiltration and activation and elevated expression of interferon signaling[5].

References:
[1] Miller K D, Pniewski K, Perry C E, et al. Targeting ACSS2 with a transition-state mimetic inhibits triple-negative breast cancer growth[J]. Cancer research, 2021, 81(5): 1252-1264.
[2] Miller K D, Schug Z T. Targeting acetate metabolism: Achilles’ nightmare[J]. British journal of cancer, 2021, 124(12): 1900-1901.
[3] Hlavaty S I, Salcido K N, Pniewski K A, et al. ACSS1-dependent acetate utilization rewires mitochondrial metabolism to support AML and melanoma tumor growth and metastasis[J]. Cell reports, 2024, 43(12).
[4] Esquea E M, Ciraku L, Young R G, et al. Selective and brain-penetrant ACSS2 inhibitors target breast cancer brain metastatic cells[J]. Frontiers in pharmacology, 2024, 15: 1394685.
[5] Miller K D, O’Connor S, Pniewski K A, et al. Acetate acts as a metabolic immunomodulator by bolstering T-cell effector function and potentiating antitumor immunity in breast cancer[J]. Nature cancer, 2023, 4(10): 1491-1507.

VY-3-135是一种强效且具有口服稳定性的ACSS2抑制剂，IC50值为44±3.85nM，水溶性为21.7μM[1]。VY-3-135目前被应用于抗乳腺癌研究及衍生物筛选实验[2-3]。

在体外，使用100μM浓度的VY-3-135处理48小时能显著抑制MDA-MB-231BR细胞和4T1细胞的增殖与存活[4]。

在体内，通过每日100mg/kg剂量的口服灌胃给药持续30天，VY-3-135在乳腺癌移植瘤小鼠模型中表现出显著的肿瘤生长抑制效果，并明显提高生存率，增强免疫细胞浸润与活化，同时上调干扰素信号通路表达[5]。

实验参考方法 Experimental Reference Method

Cell experiment [1]:

Cell lines

MDA-MB-231BR cells

Preparation Method

To assess colony formation survival, 1×105MDA-MB-231BR cells were seeded in 6-well plates until cell confluence reached 70% to 80% and then treated with 100μM VY-3-135 for 24, 48, and 72h, respectively. Cells were digested with trypsin and counted with a blood cell counting plate. A total of 1 × 104cells per treatment were seeded in 6-well plates containing fresh medium and cultured for 24h. After 24h of culture, cells were washed twice with PBS, stained with crystal violet for 30min, and washed twice more with distilled water. Colonies larger than 50 microns were counted. For crystal violet staining, 0.5% crystal violet was dissolved in a 1:1 methanol-water solution.

Reaction Conditions

100μM; 24, 48, 72h

Applications

VY-3-135 significantly inhibited the viability of MDA-MB-231BR cells in a time-dependent manner.
Animal experiment [2]:

Animal models

BALB/c mice

Preparation Method

Overall, 2.5×104T11 cells were dissolved in 100μl PBS and injected into the subcutaneous hypochondrium of 12-week-old female BALB/c mice. Mice were randomized to receive vehicle (10% dimethyl sulfoxide, 20% solotol, and 70% water with 0.5%Tween-20) by intraperitoneal (ip) injection and 100mg/kg of VY-3-135 by oral gavage daily starting the day after tumor injection. The whole procedure lasted for 30 days. Tumors were measured with calipers three times a week, and tumor volume was calculated as the weekly mean of (L × W2)/2 (where L is the longer of the two measurements). At the end of the study, all tumors were excised, snap-frozen in liquid nitrogen and stored at −80°C for downstream analysis, or immediately stored in formalin for further analysis and processing. 

Dosage form

100mg/kg/day for 30 days; p.o.

Applications

VY-3-135 treatment significantly suppressed tumor growth and significantly improved the survival rate of mice.

References:
[1] Esquea E M, Ciraku L, Young R G, et al. Selective and brain-penetrant ACSS2 inhibitors target breast cancer brain metastatic cells[J]. Frontiers in pharmacology, 2024, 15: 1394685.
[2] Miller K D, O’Connor S, Pniewski K A, et al. Acetate acts as a metabolic immunomodulator by bolstering T-cell effector function and potentiating antitumor immunity in breast cancer[J]. Nature cancer, 2023, 4(10): 1491-1507.

产品文档 Product Documents

Purity:>99.00%

化学性质Chemical Properties

CAS 号
1824637-41-3
分子式
C26H27N3O3
分子量
429.51 g/mol
溶解性
DMSO : 100 mg/mL (232.82 mM; Need ultrasonic)
保存条件
4°C, protect from light
General tips
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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
为了提高溶解度，请将管子加热至 37°C，然后在超声波浴中震荡一段时间。
Shipping Condition
评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备 RT，或根据请求配备蓝冰。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

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