GLPBio

VY-3-135

Catalog No.: GC64681Purity:>99.00%
COASDSData Sheet
يعتبر VY-3-135 مثبطًا قويًا ونشطًا عن طريق الفم ومستقرًا لـ ACSS2 بقيمة IC50 تبلغ 44 نانومترVY-3-135 خاص بـ ACSS2 بين عائلة إنزيمات AcCoA synthetaseلا يمنع VY-3-135 النشاط الأنزيمي ACSS1 أو ACSS3يمكن استخدام VY-3-135 لأبحاث سرطان الثدي

المنتجات مخصصة للاستخدام البحثي فقط، وليست للاستخدام البشري. نحن لا نبيع للمرضى.

VY-3-135
Cas No.: 1824637-41-3
10mM (in 1mL DMSO)In Stock
$132.00
1
1mgIn Stock
$70.00
1
5mgIn Stock
$140.00
1
10mgIn Stock
$224.00
1
25mgIn Stock
$364.00
1
Tel: (909) 407-4943 / (909) 689-7124Email: sales@glpbio.com

المراجع (Citations)

لا تتوفر حاليًا مراجع لهذا المنتج. فيما يلي مجموعة مختارة من المنشورات التي تستشهد بمنتجات GlpBio.
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    Nature
    641, 529–536 (2025)
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    618, 1017–1023 (2023)
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    Nature
    610, 366–372 (2022)
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    Cell
    187(9):2288-2304 (2024)
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    Cell
    183(7):1867-1883 (2020)
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    Science
    388(6745) (2025)
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    33, 904–922 (2023)
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    Cell Research
    31, 1291–1307 (2021)

الوصف (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.

البروتوكول (Protocol)

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.

وثائق المنتج (Product Documents)

Purity:>99.00%Appearance:A solid
COASDSData Sheet

الخصائص الكيميائية (Chemical Properties)

رقم CAS
1824637-41-3
الصيغة الجزيئية
C26H27N3O3
الوزن الجزيئي
429.51
الذوبانية
DMSO : 100 mg/mL (232.82 mM; Need ultrasonic)
التخزين
4°C, protect from light
إرشادات عامة
اختر مذيبًا مناسبًا وفقًا لبيانات ذوبانية المنتج. بعد التحضير، قسّم المحلول المخزون إلى أجزاء لتجنب دورات التجميد والذوبان المتكررة.
استخدم المحاليل المخزونة خلال 6 أشهر عند حفظها في -80°C، أو خلال شهر واحد عند حفظها في -20°C.
لتحسين الذوبانية، سخّن الأنبوب إلى 37°C وعرّضه للموجات فوق الصوتية لمدة مناسبة.
شروط الشحن
تُشحن عينات التقييم مع عبوات تبريد. وتُشحن الأحجام الأخرى المتاحة في درجة حرارة الغرفة، أو مع عبوات تبريد عند الطلب.

الحاسبات (Calculators)المولارية / التخفيف / الوزن الجزيئي / تحويل الوحدات / تركيبة داخل الجسم الحي / الذوبانية

g/mol

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