VY-3-135
目录号 : GC64681
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。
Cas No.:1824637-41-3
Sample solution is provided at 25 µL, 10mM.
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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]。
| 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: | |
| Cas No. | 1824637-41-3 | SDF | Download SDF |
| 分子式 | C26H27N3O3 | 分子量 | 429.51 |
| 溶解度 | DMSO : 100 mg/mL (232.82 mM; Need ultrasonic) | 储存条件 | 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℃，然后在超声波浴中震荡一段时间。 |
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| 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。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.3282 mL | 11.6412 mL | 23.2823 mL |
| 5 mM | 0.4656 mL | 2.3282 mL | 4.6565 mL |
| 10 mM | 0.2328 mL | 1.1641 mL | 2.3282 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet