2. PROTAC Cell Cycle/DNA Damage Apoptosis
  3. PROTACs DNA/RNA Synthesis Apoptosis
  4. LC-1-40

LC-1-40 是一种 PROTAC，能选择性降解 NUDT1 (DC50=0.97 nM)。LC-1-40 在小鼠模型中，能选择性抑制 MYCN 引起的肿瘤生长。LC-1-40 还能诱导 MYCN 相关性肿瘤的核苷酸损伤和细胞凋亡 (apoptosis)。LC-1-40 可用于癌症的研究。(Red: NUDT1 binder; Blue: CRBN ligand; Black: Linker)。

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LC-1-40 Chemical Structure

LC-1-40 Chemical Structure

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LC-1-40 相关抗体

Top Publications Citing Use of Products

查看 PROTACs 亚型特异性产品:

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

LC-1-40 is a PROTAC that selectively degrades NUDT1 (DC50=0.97 nM). LC-1-40 selectively inhibits MYCN-induced tumor growth in mouse models. LC-1-40 also induces nucleotide damage and apoptosis in MYCN-associated tumors. LC-1-40 can be used in cancer research[1]. (Red: NUDT1 binder; Blue: CRBN ligand; Black: Linker).

IC50 & Target

DC50: 0.97 nM (NUDT1)[1].
体外研究
(In Vitro)

LC-1-40 (0.1, 1, 10, 50, 100 µM; 0.5, 1, 2, 4, 6 h) 在 SHEP MYCN-ER 细胞中，能有效地以剂量和时间依赖性的方式诱导 NUDT1 降解[1]。

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

LC-1-40 相关抗体:

Western Blot Analysis[1]

Cell Line: SHEP MYCN-ER cells
Concentration: 0.1, 1, 10, 50, 100 µM
Incubation Time: 0.5, 1, 2, 4, 6 h
Result: Induced NUDT1 degradation in a dose- and time-dependent manner.
体内研究
(In Vivo)

LC-1-40 (30 mg/kg; i.p.; once daily for 15 days) 在小鼠体内，选择性抑制 NUDT1 相关性肿瘤的生长[1]。
1.19 LC-1-40 在雄性 C57BL/6 小鼠中的药代动力学参数[1]。

IV (5 mg/kg) IP (30 mg/kg) PO (30 mg/kg)
T1/2 (h) 6.34 42.7 7.13
Tmax (h) 0.08 3.33 3.33
Cmax (ng/mL) 4373 3080 1923
AUCInf (h*ng/mL) 32571 59799 25063
CL (mL/min/kg) 2.57 - -
Vss (mL/kg) 1.2 - -
F (%) - 32.7 14.2

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

Animal Model: T409 xenografts model[1].
Dosage: 30 mg/kg
Administration: Intraperitoneal injection; once daily for 15 days
Result: Inhibited the growth of NUDT1-related tumor.
Animal Model: Male C57BL/6 mice[1].
Dosage: 50 mg/kg, 30 mg/kg
Administration: Intravenous/Intraperitoneal/Oral; single dose
Result: Exhibited an oral bioavailability of 14.2%, nominating it as a promising lead for further optimization
分子量

844.96

Formula

C49H48N8O6
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

LC-1-40 相关分类

  • 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)

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
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:

LC-1-40PROTACsDNA/RNA SynthesisApoptosiscancertumorCRISPR-Cas9MYCNOX4PLK1KellySF188Inhibitorinhibitorinhibit

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目录号：
HY-158062
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