Sunitinib malate (cas 341031-54-7)
- CAS：341031-54-7
- Indications: Gastrointestinal stromal cancer, advanced renal cell carcinoma
- Pharmacology: Small molecules that can inhibit multiple receptor tyrosine kinases (RTK), some of which are involved in tumor growth, pathological blood vessel formation, and tumor metastasis.
Compound Information: Sunitinib Malate
| Category | Details |
|---|---|
| Name | Sunitinib Malate |
| CAS Number | 341031-54-7 |
| Synonyms | SUTENT; N-(2-(Diethylamino)ethyl)-5-((Z)-(5-fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidene)methyl)-2,4-dimethyl-1H-pyrrole-3-carboxamide (2S)-hydroxybutanedioate |
| EINECS Number | 638-825-9 |
| Molecular Formula | C₂₂H₂₇FN₄O₂·C₄H₆O₅ |
| Molecular Weight | 532.56 g/mol |
| Chemical Properties | |
| – Melting Point | 189–191°C |
| – Storage Temp. | Store at +4°C |
| – Solubility | >10 mg/mL in DMSO |
| – Form | Orange powder |
| – Color | Orange |
| – Stability | Stable for 2 years as supplied; DMSO solutions stored at -20°C for ≤3 months |
| InChIKey | XGQXULJHBWKUJY-LYIKAWCPSA-N |
| SMILES | C@@H(C(=O)O)CC(=O)O.C(/C1NC(C)=C(C(=O)NCCN(CC)CC)C=1C)=C1/C(NC2=CC=C(F)C=C/12)=O |
Key Notes:
- Chemical Structure:
- A methanesulfonate salt of sunitinib, a multi-kinase inhibitor targeting VEGFR, PDGFRβ, KIT, and FLT3.
- Contains a fluorinated indole core and a pyrrole-carboxamide moiety for enhanced target binding.
- Pharmacological Role:
- Oral administration for advanced cancers (e.g., renal cell carcinoma, gastrointestinal stromal tumors).
- Inhibits angiogenesis and tumor proliferation via VEGFR2/3 and PDGFRβ blockade.
- Clinical Use:
- Approved indications:
- Advanced renal cell carcinoma (RCC).
- Imatinib-resistant gastrointestinal stromal tumors (GIST).
- Pancreatic neuroendocrine tumors (pNET).
- Dosage: 50 mg daily (4 weeks on/2 weeks off) for RCC/GIST; 37.5 mg daily for pNET.
- Approved indications:
- Safety & Toxicity:
- Common side effects: Fatigue, diarrhea, hypertension, hand-foot syndrome.
- Severe risks: Liver toxicity, QT prolongation, thrombocytopenia.
- Supplier Information:
- Pricing: ~$0.5–5/mg (varies by purity and order volume).
Analytical & Handling Guidelines:
- Detection: HPLC-MS for purity and metabolite analysis.
- Stability: Store under inert atmosphere; avoid light and humidity.
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