Chemical Property of Napabucasin
Chemical Property:
- Melting Point:225-226℃ (dichloromethane )
- Boiling Point:444.4±45.0 °C(Predicted)
- Density:1.385±0.06 g/cm3(Predicted)
- Storage Temp.:+2C to +8C
- Solubility.:Soluble in DMSO (up to 20 mg/ml)
- XLogP3:2.3
- Hydrogen Bond Donor Count:0
- Hydrogen Bond Acceptor Count:4
- Rotatable Bond Count:1
- Exact Mass:240.04225873
- Heavy Atom Count:18
- Complexity:414
- Purity/Quality:
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98%,99%, *data from raw suppliers
Napabucasin *data from reagent suppliers
Safty Information:
- Pictogram(s):
- Hazard Codes:
- MSDS Files:
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SDS file from LookChem
Useful:
- Canonical SMILES:CC(=O)C1=CC2=C(O1)C(=O)C3=CC=CC=C3C2=O
- Recent ClinicalTrials:BBI608 and Best Supportive Care vs Placebo and Best Supportive Care in Pretreated Advanced Colorectal Carcinoma
- Recent EU Clinical Trials:A Phase II/III Randomized, Open-Label Clinical Study of Napabucasin in Combination with Weekly Paclitaxel and Low-dose Gemcitabine in Patients With Metastatic Pancreatic Cancer Following Chemotherapy Failure
- Recent NIPH Clinical Trials:Clinical pharmacology study of BBI608
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Description
Napabucasin is an inhibitor of cancer cell stemness. It reduces growth in a panel of cancer cells enriched for high stemness (IC50s = 0.291-1.249 μM) and decreases protein and gene expression of various self-renewal and pro-survival markers including Nanog, Smo, Axl, Atm, and Bmi-1 in a concentration-dependent manner in FaDu head and neck squamous cell carcinoma (HNSCC) cells. In vivo, napabucasin (20 mg/kg per day) inhibits tumor growth in a PaCa-2 mouse xenograft model and prevents tumor regrowth after cessation of treatment. It blocks formation of spleen and liver metastases in an HT29 intrasplenic nude mouse model system (ISMS) model. Napabucasin (40 mg/kg, i.p.) also reduces tumor volume in PC3 and 22RV1 prostate cancer mouse xenograft models.
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Uses
Napabucasin is a cancer cell stemness inhibitor which attenuates the progression of prostate cancer.
