规格

价格

库存

数量

1 mg

¥ 1,630

现货

5 mg

¥ 3,630

现货

10 mg

¥ 5,170

现货

25 mg

¥ 7,830

现货

50 mg

¥ 10,500

现货

1 mL x 10 mM (in DMSO)

¥ 4,820

现货

生物活性

产品描述	TNG348 is an allosteric, selective, and reversible inhibitor of USP1, causing dose-dependent accumulation of ubiquitinated substrates in vitro and in vivo. CRISPR screens demonstrate that TNG348 disrupts DNA damage tolerance by interfering with the translesion synthesis pathway via RAD18-dependent ubiquitinated PCNA. Although both TNG348 and PARP inhibitors selectively kill homologous recombination-deficient tumors, they act through distinct mechanisms: PARP1 knockout confers resistance to PARP inhibitors but sensitizes cells to TNG348. Consistent with this mechanistic divergence, combining TNG348 with PARP inhibitors results in synergistic antitumor efficacy, including tumor growth inhibition and regression in multiple HRD mouse xenograft models.
体外活性	TNG348在体外对USP1表现出高选择性抑制活性，IC50值为98.5 nmol/L。通过冷冻电镜结构测定，发现TNG348结合在USP1的一个隐秘变构口袋中，非竞争性地抑制USP1的活性 [1]。在MDA-MB-436细胞中，TNG348剂量依赖性地积累泛素化的PCNA和FANCD2，IC50值为98.6 nmol/L [1]。
体内活性	在MDA-MB-436肿瘤小鼠模型中，TNG348以30 mg/kg每天或20 mg/kg每天两次的剂量口服给药，显示出良好的药代动力学特性，血浆暴露量高于体外IC50值超过8小时 [1]。
别名	TNG-348, TNG 348

化学信息

分子量	603.52
分子式	C₂₇H₂₃F₆N₉O
CAS No.	2839740-79-1
Smiles	FC(F)(F)C=1N=C(C=2C=CC(=CC2)CN3C4=NC(=NC=C4N(C3=N)CC(F)(F)F)C=5C(=NC=NC5C6CC6)OC)N(C1)C

储存&溶解度

存储

Store at low temperature Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

实际储存温度请以COA为准

溶解度信息

DMSO: 80 mg/mL (132.56 mM), Sonication is recommeded.

溶液配制表

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.6569 mL	8.2847 mL	16.5695 mL	82.8473 mL
5 mM	0.3314 mL	1.6569 mL	3.3139 mL	16.5695 mL
10 mM	0.1657 mL	0.8285 mL	1.6569 mL	8.2847 mL
20 mM	0.0828 mL	0.4142 mL	0.8285 mL	4.1424 mL
50 mM	0.0331 mL	0.1657 mL	0.3314 mL	1.6569 mL
100 mM	0.0166 mL	0.0828 mL	0.1657 mL	0.8285 mL

该溶液配制表仅适用于固体产品。对于液体产品，请根据标明的浓度或密度计算稀释方案。

TNG348

TNG348

产品介绍

引用文献

计算器

体内实验配液计算器

剂量转换

TNG348

TNG348

TNG348 相关产品

产品介绍

引用文献

计算器

体内实验配液计算器

剂量转换