XIAP/cIAP1 antagonist-1
XIAP/cIAP1 antagonist-1 is a potent and orally active XIAP/cIAP1 antagonist with EC50s of 5.1 nM and 0.32 nM for XIAP and cIAP1, respectively. XIAP/cIAP1 antagonist-1 inhibits the tumor growth in dose-dependent manner in vivo.
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- CAS. Nr.: 1403898-55-4
- Formel: C29H40FN5O2
- Molecular Weight:509.66
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
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XIAP 5.1 nM (IC50) |
cIAP1 0.32 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| MDA-MB-231 | EC50 |
4.4 nM
Compound: 26
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Cytotoxicity against human MDA-MB-231 cells assessed as decrease in cell proliferation after 72 hrs by alamar blue assay
Cytotoxicity against human MDA-MB-231 cells assessed as decrease in cell proliferation after 72 hrs by alamar blue assay
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[PMID: 28492317] |
| MDA-MB-231 | IC50 |
4.4 nM
Compound: 5; AT-IAP
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Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by Alamar blue assay
Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by Alamar blue assay
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[PMID: 30091600] |
XIAP/cIAP1 antagonist-1 (compound 26) shows antiproliferation activity in MDA-MB-231 cells witn an IC50 value of 4.4 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
XIAP/cIAP1 antagonist-1 (1 mg/kg for i.v.; 5, 30 mg/kg for p.o.) shows oral bioavailability (F=22%) at 5 mg/kg[1].
Pharmacokinetic Parameters of XIAP/cIAP1 antagonist-1 in Balb/c SCID mice[1].
| dose (mg/kg) | route | Tmax (h) | Cmax (µg/mL) | CLp (mL/min/kg) | Vss (L/kg) | half life (h) | AUC (µg·h/mL) | F (%) |
| 1 | IV | 40.9 | 6.4 | 3.0 | 0.41 | |||
| 5 | PO | 2 | 0.12 | 1.8 | 0.45 | 22 | ||
| 30 | PO | 1 | 1.7 | 12.1 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Balb/c SCID mice bearing MDA-MB-231 xenografts[1]
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Dosage:7.5, 15, 30 mg/kg
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Administration:PO; daily for 24 days
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Result:Inhibited the tumor growth in dose-dependent manner.
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Animal Model:Balb/c SCID mice bearing MDA-MB-231 xenografts[1]
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Dosage:
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Administration:1 mg/kg for i.v.; 5, 30 mg/kg for p.o.
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Result:Showed oral bioavailability (F=22%).
Chemical Information
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CAS. Nr. 1403898-55-4
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Appearance Solid
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Molecular Weight 509.66
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Formel C29H40FN5O2
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Color White to off-white
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SMILES
C[C@H]1N(C[C@@H]2N(CC(N3CC(C)(C)C4=NC=C(CC5=CC=C(F)C=C5)C=C43)=O)C[C@@H](C)NC2)CCOC1
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
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Data Sheet (275 KB)
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SDS (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
XIAP/cIAP1 antagonist-1 Related Classifications
HY-102051 Related Classifications
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