INCB3619 structure
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Common Name | INCB3619 | ||
|---|---|---|---|---|
| CAS Number | 791826-72-7 | Molecular Weight | 413.46700 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C22H27N3O5 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of INCB3619INCB3619 is a selective and orally active ADAM inhibitor with IC50 of 22 nM and 14 nM for ADAM10 and ADAM17, respectively. INCB3619 has anti-tumor activity[1]. |
| Name | methyl (6S,7S)-7-(hydroxycarbamoyl)-6-(4-phenyl-3,6-dihydro-2H-pyridine-1-carbonyl)-5-azaspiro[2.5]octane-5-carboxylate |
|---|---|
| Synonym | More Synonyms |
| Description | INCB3619 is a selective and orally active ADAM inhibitor with IC50 of 22 nM and 14 nM for ADAM10 and ADAM17, respectively. INCB3619 has anti-tumor activity[1]. |
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| Related Catalog | |
| In Vitro | INCB3619 (0-0.25 μM, 96 h) 可以抑制 heregulin 依赖性 HER3-Akt 通路,但不能抑制 A549 细胞中的 ERK 活性,可诱导 A549 细胞凋亡[1]。 INCB3619 (0-10 μM, 72 h) 可以抑制 EGFR 自分泌细胞系 NCI-H1666 中的 EGFR 配体信号传导,并可与其他抗 EGFR 药物,如吉非替尼联合使用[1]。 INCB3619 (2 µM) 抑制 NCI-H166 细胞中 ERK1/2 的表达,使其对吉非替尼 (Gefitinib,HY-50895) 敏感[1]。 Apoptosis Analysis[1]. Cell Line: A549 cell Concentration: 1, 10 μM Incubation Time: Result: Induced about 3% apoptosis at a concentration of 1 μM and about 5% at a concentration of 10 μM. Cell Viability Assay[1]. Cell Line: NCI-H1666 cell Concentration: 0-10 μM Incubation Time: 72 h Result: Inhibited proliferation of NCI-H1666 cells. |
| In Vivo | INCB3619 (subcutaneous injection,60 mg/kg/d,14 d) 在 A549 异种移植的 BALB/c nu/nu 小鼠模型中,具有抗肿瘤活性,并使肿瘤对吉非替尼 (Gefitinib,HY-50895) 敏感[1]。 Animal Model: BALB/c nu/nu mouse model of A549 xenograft Dosage: 50, 60 mg/kg Administration: subcutaneous injection, daily, 14 d Result: Significant tumor growth inhibition and delay at 60 mg/kg dose, less active effect at 50 mg/kg. |
| References |
| Molecular Formula | C22H27N3O5 |
|---|---|
| Molecular Weight | 413.46700 |
| Exact Mass | 413.19500 |
| PSA | 102.67000 |
| LogP | 2.76090 |
| InChIKey | CKZHFOKQZRZCPF-ROUUACIJSA-N |
| SMILES | COC(=O)N1CC2(CC2)CC(C(=O)NO)C1C(=O)N1CC=C(c2ccccc2)CC1 |
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Name: Inhibition of MMP14
Source: ChEMBL
Target: Matrix metalloproteinase-14
External Id: CHEMBL1002951
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Name: Inhibition of TACE
Source: ChEMBL
Target: Disintegrin and metalloproteinase domain-containing protein 17
External Id: CHEMBL1002953
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Name: Inhibition of MMP9
Source: ChEMBL
Target: Matrix metalloproteinase-9
External Id: CHEMBL1002949
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Name: Protein binding in murine plasma
Source: ChEMBL
Target: Mus musculus
External Id: CHEMBL911380
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Name: AUC (0-24h) in murine at 10 mg/kg, po
Source: ChEMBL
Target: Mus musculus
External Id: CHEMBL911381
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Name: Inhibition of MMP12
Source: ChEMBL
Target: Macrophage metalloelastase
External Id: CHEMBL1002955
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Name: Decrease of tumor volume in CD1 mouse xenografted with BT474 cells overexpressing HER...
Source: ChEMBL
Target: Receptor tyrosine-protein kinase erbB-2
External Id: CHEMBL911383
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Name: Inhibition of ADAM10
Source: ChEMBL
Target: Disintegrin and metalloproteinase domain-containing protein 10
External Id: CHEMBL953083
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| incb 3619 |
| unii-q56ue7e40y |