1. Cell Cycle/DNA Damage Apoptosis
  2. DNA/RNA Synthesis Apoptosis
  3. Thailanstatin D

Thailanstatin D 是 Thailanstatin A 的类似物,通过干扰 U2AF65 和 SAP155 之间的相互作用,阻止它们与位于分支点和 3' 剪接位点之间的多嘧啶束结合,能够抑制 AR-V7 基因剪接。Thailanstatin D 对人 CRPC 异种移植瘤具有明显的抑瘤作用,可导致细胞凋亡 (apoptosis)。

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Thailanstatin D Chemical Structure

Thailanstatin D Chemical Structure

CAS No. : 1609105-89-6

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Thailanstatin D, an analogue of Thailanstatin A, is able to inhibit AR-V7 gene splicing by interfering the interaction between U2AF65 and SAP155 and preventing them from binding to polypyrimidine tract located between the branch point and the 3' splice site. Thailanstatin D exhibits a potent tumor inhibitory effect on human CRPC xenografts leading to cell apoptosis[1].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
BT-474 IC50
4.8 nM
Compound: 4
Cytotoxicity against human BT474 cells after 4 days by MTS/cell proliferation assay
Cytotoxicity against human BT474 cells after 4 days by MTS/cell proliferation assay
[PMID: 25098528]
MDA-MB-468 IC50
3.4 nM
Compound: 4
Cytotoxicity against human MDA-MB-468 cells after 4 days by MTS/cell proliferation assay
Cytotoxicity against human MDA-MB-468 cells after 4 days by MTS/cell proliferation assay
[PMID: 25098528]
NCI-H1975 IC50
3.6 nM
Compound: 4
Cytotoxicity against human NCI-H1975 cells after 4 days by MTS/cell proliferation assay
Cytotoxicity against human NCI-H1975 cells after 4 days by MTS/cell proliferation assay
[PMID: 25098528]
NCI-N87 IC50
2 nM
Compound: 4
Cytotoxicity against human NCI-N87 cells after 4 days by MTS/cell proliferation assay
Cytotoxicity against human NCI-N87 cells after 4 days by MTS/cell proliferation assay
[PMID: 25098528]
体外研究
(In Vitro)

Thailanstatin D (0-50 nM; 4 hours) significantly decreases the protein levels of AR-V7 and other AR-Vs (AR splice variants)[1].

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

Cell Viability Assay[1]

Cell Line: VCaP, 22RV1 and LN95 cells
Concentration: 0-50 nM
Incubation Time: 4 hours
Result: The mRNA levels of both AR-V7 and AR-FL were suppressed by Thailanstatin D in a dose-dependent manner.
体内研究
(In Vivo)

Thailanstatin D (300 µg/kg; ALZET osmotic pumps; daily for 4 days) significantly inhibits the tumor growth[1].

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

Animal Model: NOD-SCID mice ( Mice bearing 22RV1 xenografts)[1]
Dosage: 300 µg/kg
Administration: ALZET osmotic pumps; daily for 4 days
Result: Significantly inhibited the tumor growth.
分子量

519.63

Formula

C28H41NO8

CAS 号
结构分类
初始来源

Burkholderia thailandensis

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
  • 摩尔计算器

  • 稀释计算器

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质量   浓度   体积   分子量 *
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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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.

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Thailanstatin D
目录号:
HY-139104
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