2. Cell Cycle/DNA Damage Cytoskeleton Apoptosis
  3. Microtubule/Tubulin Apoptosis
  4. Tubulin-IN-54

Tubulin-IN-54 is a tubulin inhibitor. Tubulin-IN-54 exhibits anti-proliferative activity against various cancer cells. Tubulin-IN-54 inhibits tubulin polymerization, disrupts microtubule networks, induces G2/M cell cycle arrest, and promotes cancer cell apoptosis. Tubulin-IN-54 demonstrates significant anti-tumor efficacy in mice bearing PC-3/TxR xenografts. Tubulin-IN-54 can be used for the study of taxane-resistant cancers (prostate cancer, melanoma).

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Tubulin-IN-54

Tubulin-IN-54 構造式

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Tubulin-IN-54 関連抗体

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製品説明

Tubulin-IN-54 is a tubulin inhibitor. Tubulin-IN-54 exhibits anti-proliferative activity against various cancer cells. Tubulin-IN-54 inhibits tubulin polymerization, disrupts microtubule networks, induces G2/M cell cycle arrest, and promotes cancer cell apoptosis. Tubulin-IN-54 demonstrates significant anti-tumor efficacy in mice bearing PC-3/TxR xenografts. Tubulin-IN-54 can be used for the study of taxane-resistant cancers (prostate cancer, melanoma)[1].

体外実験

Tubulin-IN-54 (Compound 11b) (72 h) exhibits potent anti-proliferative activity against human melanoma A375 (IC50 = 0.6 nM), M14 (IC50 = 0.6 nM) and human prostate cancer PC-3 (IC50 = 1.3 nM) cells[1].
Tubulin-IN-54 (2-5 nM, 24 h) inhibits tubulin polymerization and disrupts microtubule network structures in PC-3/TxR cells[1].
Tubulin-IN-54 (0.5-5 nM, 24 h) potently inhibits colony formation and migration of PC-3/TxR cells[1].
Tubulin-IN-54 (1-5 nM, 24 h) induces G2/M cell cycle arrest and apoptosis in PC-3/TxR cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Tubulin-IN-54 関連抗体

Cell Migration Assay [1]

Cell Line: PC-3/TxR cells
Concentration: 1, 2, 5 nM
Incubation Time: 24 h
Result: Inhibited migration of PC-3/TxR cells.

Cell Cycle Analysis[1]

Cell Line: PC-3/TxR cells
Concentration: 1, 2, 5 nM
Incubation Time: 24 h
Result: Induced G2/M cell cycle arrest in PC-3/TxR cells.

Apoptosis Analysis[1]

Cell Line: PC-3/TxR cells
Concentration: 1, 2, 5 nM
Incubation Time: 24 h
Result: Induced apoptosis in PC-3/TxR cells.
Downregulated the expression of anti-apoptotic protein Bcl-2.
Upregulated the expression of pro-apoptotic proteins cleaved-PARP and cleaved-caspase-3.
体内実験

Tubulin-IN-54 (Compound 11b) (15 mg/kg, i.p., 5 times/week for 2 weeks) demonstrates significant anti-tumor efficacy in NSG male mice bearing PC-3/TxR prostate cancer xenografts[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: PC-3/TxR cells (2.5 × 106 in 100 µL mixture of medium and Matrigel at 1:1 ratio) were subcutaneously implanted into the dorsal right flanks of 8-9-week-old male NOD scid gamma (NSG) mice[1]
Dosage: 15 mg/kg
Administration: i.p. 5 times/week for 2 weeks
Result: Achieved tumor growth inhibition (TGI) rates of 67% and 80% at doses of 15 mg/kg and 30 mg/kg.
Reduced the Ki67 expression.
Induced increased phosphorylation of Histone H3 (a G2/M phase arrest marker).
Increased the expression of cleaved-PARP and cleaved-caspase-3.
Reduced the expression of CD31 (a vascular marker).
Showed no acute toxicity to major organs (liver, lung, spleen, kidney).
分子量

377.39

分子式

C21H19N3O4
SMILES

O=C(C1=CC(OC)=C(C(OC)=C1)OC)C2=NC(C3=CC=CC4=C3C=CN4)=CN2
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
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Tubulin-IN-54 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Tubulin-IN-54Microtubule/TubulinApoptosisPC-3/TxRtubulinprostate cancermelanomaapoptosisInhibitorinhibitorinhibit

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製品名:
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製品番号:
HY-175555
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