1. Cell Cycle/DNA Damage
    Epigenetics
  2. PARP
  3. RK-287107

RK-287107 

目录号: HY-123892
产品使用指南

RK-287107 是一种有效的特异性 tankyrase 抑制剂,抑制 tankyrase-1tankyrase-2IC50 分别为 14.3 和 10.6 nM。RK-287107 可阻断结直肠癌细胞生长。

MCE 的所有产品仅用作科学研究,我们不为任何个人用途提供产品和服务

RK-287107 Chemical Structure

RK-287107 Chemical Structure

CAS No. : 2171386-10-8

1.  客户无需承担相应的运输费用。

2.  同一机构(单位)同一产品试用装仅限申领一次,同一机构(单位)一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户

Size Stock
250 mg Get quote
500 mg Get quote

* Please select Quantity before adding items.

Customer Review

Top Publications Citing Use of Products
  • 生物活性

  • 技术信息

  • 纯度 & 产品资料

  • 参考文献

Description

RK-287107 is a potent and specific tankyrase inhibitor with IC50s of 14.3 and 10.6 nM for tankyrase-1 and tankyrase-2, respectively. RK-287107 blocks colorectal cancer cell growth[1].

IC50 & Target[1]

tankyrase-1

14.3 nM (IC50)

tankyrase-2

10.6 nM (IC50)

In Vitro

RK-87107 (0.01-10 μM; 12 hours) shows an antiproliferative effect on colorectal cancer cells harboring short adenomatous polyposis coli (APC) mutations. The 50% growth inhibition (GI50) value of RK-287107 on COLO-320DM cells is 0.449 μM[1].
RK-287107 (0.03-10 μM; 16 hours) causes accumulation of tankyrase and Axin1/2[1].
RK-287107 (0.03-10 μM; 16 hours) also downregulates β-catenin signaling in cultured cells[1].

Cell Proliferation Assay[1]

Cell Line: Colorectal cancer COLO-320DM, SW403, RKO, HCC2998, HCT-116, and DLD-1 cells
Concentration: 0.01, 0.1, 1, 10 μM
Incubation Time: 12 hours
Result: Inhibited the growth of APC-mutated (β-catenin-dependent) colorectal cancer COLO-320DM and SW403 cells. The GI50 value of RK-287107 on COLO-320DM is 0.449 μM. Did not inhibit the growth of APC-wild (β-catenin-independent) colorectal cancer cell lines, including RKO, HCT-116, HCC2998 and DLD-1.

Western Blot Analysis[1]

Cell Line: COLO-320DM cells
Concentration: 0.03, 0.1, 0.33, 1, 3, and 10 μM
Incubation Time: 16 hours
Result: Downregulation of active β-catenin was observed
In Vivo

RK-287107 (100 and 300 mg/kg; i.p. administration; once per day; 5-days on/ 2-days off schedule for 2 weeks) inhibits tumor growth in a mouse xenograft model[1].

Animal Model: 6-week-old female NOD.CB17-Prkdcscid/J mice with colorectal cancer COLO-320DM[1]
Dosage: 100 and 300 mg/kg
Administration: Administration i.p.; once per day; 5-days on/ 2-days off schedule for 2 weeks
Result: 100 and 300 mg/kg resulted in 32.9% and 44.2% TGI, respectively.
Storage

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

References
Molecular Weight

416.46

Formula

C₂₂H₂₆F₂N₄O₂

CAS No.

2171386-10-8

SMILES

O=C1NC(N2CCC3(CC2)CN(CCO)C4=C3C(F)=CC(F)=C4)=NC5=C1CCCC5

Shipping

Room temperature in continental US; may vary elsewhere

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

您最近查看的产品:

Your information is safe with us. * Required Fields.

   产品名称:

 

* 需求量:

* 客户姓名:

 

* Email:

* 电话:

 

* 公司或机构名称:

   留言给我们:

Bulk Inquiry

Inquiry Information

产品名称:
RK-287107
目录号:
HY-123892
需求量:

RK-287107

Cat. No.: HY-123892