GLPBio

Pracinostat (SB939)

Catalog No.: GC16734Purity:>99.50%Synonyms: Pracinostat

A pan-HDAC inhibitor

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


Pracinostat (SB939)
Cas No.: 929016-96-6
10mM (in 1mL DMSO)In Stock
$100.00
1
5mgIn Stock
$79.00
1
10mgIn Stock
$151.00
1
50mgIn Stock
$432.00
1

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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    628, 630–638 (2024)
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    632, 686–694 (2024)
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    Nature
    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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الوصف (Description)

Pracinostat, also known as SB939, is a potent and orally available inhibitor of histone deacetylase (HDAC) with a relatively stronger selectivity (more than 1000-fold) for class I, class II and class IV HDACs rather than class III HDACs. Pracinostat potently suppresses proliferation in a wide range of cancer cell lines, including colon cancer, ovarian cancer, prostate carcinomas, acute myeloid leukaemia (AML) and B cell lymphoma. Recent study results have shown that SB939 induces the accumulation of acetylated histone H3 (AcH3) and acetylated α-tubulin and increases the expression of the cyclin dependent kinase inhibitor p21 in cancer cells.

Reference

[1].Razak AR, Hotte SJ, Siu LL, Chen EX, Hirte HW, Powers J, Walsh W, Stayner LA, Laughlin A, Novotny-Diermayr V, Zhu J, Eisenhauer EA. Phase I clinical, pharmacokinetic and pharmacodynamic study of SB939, an oral histone deacetylase (HDAC) inhibitor, in patients with advanced solid tumours. Br J Cancer. 2011;104(5):756-762.

البروتوكول (Protocol)

Cell experiment:

Cell lines

Ovarian (A2780) , colon (HCT-116), and prostate (PC-3) cell lines

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months.

Reaction Conditions

96 h; IC50=0.48±0.21 μM (A2780), 0.48±0.27 μM (HCT-116), 0.34±0.06 μM (PC-3)

Applications

SB939 showed broad anti-proliferative activity against representative tumor cells from ovarian (A2780) , colon (HCT-116), and prostate (PC-3) with cellular IC50 values of 0.48±0.21, 0.48±0.27 and 0.34±0.06 μM, respectively.

Animal experiment:

Animal models

Athymic nude mice

Dosage form

200 mg/kg, 100 mg/kg, 50 mg/kg; oral taken.

Applications

SB939 was clearly toxic at the highest dose tested (200 mg/kg); however, at the MTD dose of 100 mg/kg and at 50mg/kg, it demonstrated very significant antitumor effects on day 21 with TGI = 90% (p < 0.001 ) and 66% ( p < 0.001), respectively, with acceptable body weight loss.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1] Wang H, Yu N, Chen D, et al. Discovery of (2 E)-3-{2-butyl-1-[2-(diethylamino) ethyl]-1 H-benzimidazol-5-yl}-N-hydroxyacrylamide (SB939), an orally active histone deacetylase inhibitor with a superior preclinical profile[J]. Journal of medicinal chemistry, 2011, 54(13): 4694-4720.

وثائق المنتج (Product Documents)

Purity:>99.50%Appearance:A solid

الخصائص الكيميائية (Chemical Properties)

رقم CAS
929016-96-6
المرادفات
Pracinostat
الاسم الكيميائي
(E)-3-[2-butyl-1-[2-(diethylamino)ethyl]benzimidazol-5-yl]-N-hydroxyprop-2-enamide
SMILES
CCCCC1=NC2=C(N1CCN(CC)CC)C=CC(=C2)C=CC(=O)NO
الصيغة الجزيئية
C20H30N4O2
الوزن الجزيئي
358.48
الذوبانية
≥ 11.4 mg/mL in DMSO, ≥ 24.8 mg/mL in EtOH with ultrasonic
التخزين
Store at -20°C
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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