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PF-06840003
总货号: MB3835
货号 规格 库存 发货时间
5mg [¥800.00] :¥800.00
15
现货
25mg [¥2800.00] :¥2800.00
15
现货
数量
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相关论文

PF-06840003是高度选择的有口服活性的IDO-1抑制剂。
PF-06840003 is a highly selective orally bioavailable IDO-1 inhibitor. Although it has moderate hIDO1 enzyme inhibition (IC50 0.41 μM), it is a highly efficient compound (LE 0.53, LipE 5.1), driven by its tight packing within the enzyme, as well as the high density of hydrogen bonds it forms withm hIDO-1 despite its small size.

相关谱图:

HNMR

理化数据

分子量

232.21

化学式

C12H9FN2O2
 

CAS

198474-05-4

稳定性

3 years -20°C powder

2 years -80°C in solvent

溶解性

DMSO

46 mg/mL (198.09 mM)

Ethanol

6 mg/mL (25.83 mM)

Water

Insoluble

生物活性

产品描述

PF-06840003 is a highly selective orally bioavailable IDO-1 inhibitor. Although it has moderate hIDO1 enzyme inhibition (IC50 0.41 μM), it is a highly efficient compound (LE 0.53, LipE 5.1), driven by its tight packing within the enzyme, as well as the high density of hydrogen bonds it forms withm hIDO-1 despite its small size.

靶点

hIDO-1 (Cell-free)

dIDO-1 (Cell-free)

mIDO-1 (Cell-free)

0.41 μM

0.59 μM

1.5 μM

体外研究

PF-06840003 is a racemic mixture. The IC50s of PF-06840003 for hIDO-1, mouse IDO-1 and dog IDO-1 are 0.41, 1.5 and 0.59 μM, respectively. It has very weak activity against hTDO-2, with an IC50 of 140 μM. In cellular assays, PF-06840003 shows activity both in the HeLa assay (IC50 1.8 μM) as well as in the LPS/INFγ-stimulated THP1 cells (IC50 1.7 μM). PF-06840003 is a very weak inhibitor of CYPs with IC50 values greater than 100 μM for most major CYP isozymes except 2C19 (IC50 value is 78 μM). Additionally, PF-06840003 does not exhibit metabolism-dependent (time-dependent and NADPH-dependent or time-dependent (NADPH-independent) inhibition of the major CYP enzymes investigated.

体内研究

PF-06840003 has a predicted half-life of 16−19 h. Oral bioavailability in the mouse and rat was 59 and 94%, respectively, and 19% in dog. PF-06840003 has shown significant antitumor activity in monotherapy in Pan02, B16−F10, CT26, MC38, 4T1, and Renca models (p < 0.05 vs vehicle-treated group) and very good synergy in combination with anti-PDL1 mAb in CT26 model (p < 0.05 vs monotherapy groups).The PK profile of the compound is excellent, with a low/moderate clearance in most preclinical species. The compound also shows good CNS penetration in rat, suggesting potential impact on brain metastases

实验操作(仅供参考)

细胞实验:
  • Cell lines: HeLa cervical carcinoma cells
  • Concentrations: 0-50 μM
  • Incubation Time: 16−24 h
  • Method:

HeLa cells were harvested from cell culture flasks using 0.25% trypsin/EDTA and neutralized with EMEM growth medium. Following resuspension in fresh growth media, cells were seeded at 20,000 cells per well in 200 μL growth media in a 96-well plate and allowed to adhere at 37 °C at 5% CO2 overnight. The following day, growth media was aspirated and replaced with 200 μL of reduced (2%) serum media containing 100 ng/mL recombinant human interferon gamma (rhIFNγ) and incubated at 37 °C with 5% CO2 for 48 h to induce IDO-1 expression. On day four, compounds were diluted to 10 mM in DMSO and 11-point three-fold dilutions were prepared. rhIFNγ-containing media was removed, and following dilution into EMEM, compounds were added to cells at 50 μM top concentration and allowed to incubate 16−24 h at 37 °C with 5% CO2. On day five of the assay, 100 μL of cell supernatant was transferred to a v-bottom 96-well plate. Thirty microliters of 30% trichloroacetic acid (TCA) was added to each well to precipitate proteins, and plates were centrifuged at 3000 rpm for 10 min. One hundred microliters was transferred to a fresh flat-bottom 96-well plate, and 100 μL/well of 2% 4-(dimethylamino)benzaldehyde (pDMAB) in acetic acid was added to derivatize N-formyl kynurenine to kynurenine for quantitative colorimetric readout. Assay plates were read at A492 on Envision plate reader.
(Only for Reference)

动物实验:

  • Animal Models: CD-1 mice, Wistar−Han rat, and Beagle dog
  • Formulation: PBS
  • Dosages: 1 mg/kg (IV) and 3 mg/kg (oral)
  • Administration: i.v./oral
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英文名字:EOS200271
质量标准:>98%,BR
分子式:C12H9FN2O2
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