2. Cell Cycle/DNA Damage Epigenetics
  3. PARP
  4. YCH1899

YCH1899是一种具有口服活性的PARP抑制剂，对PARP1/2的IC50均小于0.001 nM。YCH1899对Olaparib (HY-10162) 耐药和Talazoparib (HY-16106) 耐药的Capan-1细胞 (Capan-1/OP和Capan-1/TP细胞) 显示出明显的抗增殖活性，IC50值分别为0.89和1.13 nM。YCH1899在大鼠体内具有良好的药代动力学特性。

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YCH1899 Chemical Structure

YCH1899 Chemical Structure

CAS No. : 3032451-66-1

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YCH1899 相关抗体

Top Publications Citing Use of Products

查看 PARP 亚型特异性产品:

查看所有亚型
PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

YCH1899 is an orally active PARP inhibitor, with an IC50< 0.001 nM for PARP1/2. YCH1899 exhibits distinct antiproliferation activity against Olaparib (HY-10162)-resistant and Talazoparib (HY-16106)-resistant Capan-1 cells (Capan-1/OP and Capan-1/TP cells) , with IC50 values of 0.89 and 1.13 nM, respectively. YCH1899 has acceptable pharmacokinetic properties in rats[1].

IC50 & Target

PARP-1

<0.001 nM (IC50)

PARP-2

<0.001 nM (IC50)

PARP3

1.1 nM (IC50)

PARP4

1.0 nM (IC50)

TNKS1

3.8 nM (EC50)

TNKS2

12.4 nM (IC50)

PARA6

9.5 nM (IC50)

PARP-7

7.3 nM (IC50)

ARTD10/PARP10

10.8 nM (IC50)

PARA11

2.166 μM (IC50)

human PARP12

14.1 nM (IC50)

PARP14

35.914 μM (IC50)

PARP15

51.623 nM (IC50)

体外研究
(In Vitro)

YCH1899 (7天) 对Capan-1、Capan-1/OP、Capan-1/TP 细胞表现出明显的抗增殖活性，IC50 分别为0.10、0.89、1.13 nM[1]。
YCH1899 (0.001-1 nM, 4 h) 稳定PARP1-DNA复合物，抑制PARP的形成[1]。
YCH1899 (3.5 h) 对BRCA突变/野生型细胞 (V−C8, V79, HCT-15, HCC1937) 的增殖有抑制作用, IC50s 范围为1.19-44.24 nM[1]。
YCH1899 (1 μM, 24 h) 在 Capan-1、Capan-1/OP、Capan-1/TP 细胞中诱导 DNA 损伤，使 γH2AX 数量大量增加[1]。
YCH1899 (1 μM, 48 h) 在 U2OS-DR-GFP 细胞中诱导 HR (Homologous Recombination, 同源重组) 修复活性显著降低[1]。

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

YCH1899 相关抗体:

Cell Proliferation Assay[1]

Cell Line: HCC1937, HCT-15, MDA-MB-436, UWB1.289, UWB1.289+BRCA1, V–C8, V79 cells
Concentration: 0-1 μM approximately
Incubation Time: 24 h
Result: Inhibited the proliferation of BRCA-Deficient/Wild-Type Cells and IC50s value were 4.54, 44.24, 0.52, 0.02, 0.34, 1.19, 29.32nM, respectively.

Immunofluorescence[1]

Cell Line: Capan-1, Capan-1/OP cells, Capan-1/TP cells
Concentration: 0.01, 0.1, 1 μM
Incubation Time: 24 h
Result: Increased γH2AX level in a dose-dependent manner.

Western Blot Analysis[1]

Cell Line: Capan-1 and Capan-1/OP cells
Concentration: 1, 10, 100 nM
Incubation Time: 4 h
Result: Improved stability of PARP1-DNA complexes and induced chromatin-bound PARP1 accumulation in the presence of MMS (methanesulfonate).
Inhibited PARP formation in the presence of 0.1% H2O2.
体内研究
(In Vivo)

YCH1899 (5 mg/kg, 静脉给药) 在大鼠中具有中等清除力[1]。
YCH1899在MDA-MB-436/OP (6.25, 12.5和25 mg/kg, 口服给药，每天一次，持续27天) 和Capan-1/R（12.5和25 mg/kg, 口服给药，每天一次，持续21天） 异种移植小鼠肿瘤模型中克服了Talazoparib耐药，肿瘤体积显著下降[1]。

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

Animal Model: MDA-MB-436/OP xenografts and Capan-1/R-in vivo xenografts mice[1]
Dosage: 12.5 and 25 mg/kg
Administration: Oral administration
Result: Inhibited MDA-MB-436/OP xenografts tumor growth with T/C of 36.74% and 15.29% at 12.5 and 25 mg/kg
Inhibited Capan-1/R xenografts tumor growth with T/C of 48.92% and 13.87% at 12.5 and 25 mg/kg.
Animal Model: rats[1]
Dosage: 5 mg/kg
Administration: Intravenous injection
Result: Had a moderate clearance rate (24.5 mL/min/kg) and half-life (3.25 h).
分子量

549.35

Formula

C25H18BrFN6O3
CAS 号
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

YCH1899 相关分类

  • 摩尔计算器

  • 稀释计算器

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

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

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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:

YCH18993032451-66-1YCH 1899YCH-1899PARPpoly ADP ribose polymeraseHCC1937UWB1.289PARPiCapan-1 cellMDA-MB-436/OP cellsxenograft mouse tumor modelsInhibitorinhibitorinhibit

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