• All
  • Primary Antibodies
  • Conjugated Antibodies for IF
  • Conjugated Antibodies for FC
  • Secondary Antibodies
  • Antibody Labeling KitsNew
  • ELISA Kits
  • IHC Kits
  • Magnetic Cell Separation Kits
  • Cytokines & Growth Factors
  • Neutralizing/activating Antibodies
  • Nanobody-based Reagents
  • Accessory Products and Kits
  • Fusion Proteins
×
×
Host
0
Species Reactivity
0
Species Reactivity
0
Conjugate
0
Conjugate
0
Compatible Species
0
Conjugate
0

Tasquinimod

Tasquinimod (ABR-215050) 是一种口服抗血管生成剂，有潜在的抗肿瘤活性。它也是 S100A9抑制剂，与 HDAC4Zn2+结合结构域结合的 Kd 值在10到30 nM 之间。

CAS号

254964-60-8

分子式

C20H17F3N2O4

主要靶点

HDAC

仅限科研使用

Cat No : CM04435

Print datasheet

Synonyms

ABR-215050|他喹莫德

验证数据展示

  • CAS No.: 254964-60-8

    Tasquinimod
    CAS#: 254964-60-8

产品信息

Tasquinimod is a quinoline-3-carboxamide linomide analog with antiangiogenic and potential antineoplastic activities. Tasquinimod has been shown to decrease blood vessel density but the exact mechanism of action is not known. This agent has also been shown to augment the antineoplastic effects of docetaxel and androgen ablation in a murine model of prostate cancer involving human prostate cancer xenografts.

CAS号 254964-60-8
分子式 C20H17F3N2O4
主要靶点 HDAC
主要通路 表观遗传|DNA损伤和修复
分子量 406.36
纯度 98.30%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 ABR-215050|他喹莫德

靶点活性

HDAC4:10-30 nM (Kd)

体内活性

Tasquinimod (30 mg/kg/d p.o.) shows anti-angiogenic activity and thus causes tumor growth inhibition in mice bearing human and rodent prostate cancer models. [2]

体外活性

Tasquinimod inhibits tumor angiogenesis by allosteric inhibition of HDAC4/N-CoR/HDAC3 dependent deacetylation of HIF-1α. [1] Tasquinimod also targets infiltrating myeloid cells, and modulates local tumour immunity by blocking the interaction between S100A9 and its ligands receptor of advanced glycation end products and Toll-like receptor 4. [3]

溶解度

DMSO:75 mg/mL (184.6 mM),Ethanol:9 mg/mL (22.1 mM),H2O:<1 mg/mL

细胞实验

Tasquinimod is dissolved in DMSO and stored, and then diluted with appropriate media before use[3]. Two human prostate cancer cell lines, CWR-22RH and LNCaP (ATCC) are both androgen independent, but remain sensitive to androgen stimulation of growth, express PSA and a mutated androgen receptor. The hormone independent cell lines LNCaP19 and DU145 are also tested for TSP1 induction after in vitro exposure to Tasquinimod (0.1-100 μM). CWR-22RH, LNCaP and DU145 are grown in RPMI Medium 1640 containing 10% FCS and L-Glutamine mixture, while LNCAP19 is cultured in RPMI-medium with 10% hormone free (RDCC) FCS[3].

参考文献

1.Isaacs JT, et al. Cancer Res.2013, 73(4), 1386-1399.
2.Isaacs JT, et al. Prostate.2006, 66(16), 1768-1778.
3.Raymond E, et al. Cancer Chemother Pharmacol.2014, 73(1), 1-8.

The molarity calculator equation

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

质量   浓度   体积   分子量 *
=
×
×

The dilution calculator equation

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