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Catalog: | HY-15454 |
Brand: | MCE |
CAS: | 1071992-99-8 |
MDL | MFCD22124467 |
---|---|
Molecular Weight | 561.71 |
Molecular Formula | C32H43N5O4 |
SMILES | O=C([C@@H]1CC[C@@](CCN(C(CC(C)C)=O)C[C@@H]2NC([C@@H](NC)C)=O)([H])N1C2=O)NC(C3=CC=CC=C3)C4=CC=CC=C4 |
cIAP1 1.9 nM (Ki) |
cIAP2 5.1 nM (Ki) |
XIAP 66.4 nM (Ki) |
Xevinapant mimic closely the AVPI peptide in both hydrogen bonding and hydrophobic interactions with XIAP, with additional hydrophobic contacts with W323 of XIAP. Xevinapant is more sensitive to these IAPs than Smac AVPI peptide with 50-100 fold binding affinities. Xevinapant (1 μM) completely restores the activity of caspase-9, which is suppressed by 500 nM XIAP BIR3 in a cell-free system. In MDA-MB-231 cell, Xevinapant induces rapid cellular cIAP1 degradation and also pulls down the cellular XIAP protein. Xevinapant effectively inhibits lots of human cancer cell lines and shows IC 50 of 144 and 142 nM in MDA-MB-231 cell and SK-OV-3 ovarian cell, with low toxicity against normal-like human breast epithelial MCF-12F cells and primary human normal prostate epithelial cells. Xevinapant induces apoptosis in MDA-MB-231 cell by inducing activation of caspase-3 and cleavage of PARP [1] . Xevinapant displays single agent activity in ovarian cancer cell lines. The IC 50 values of AT-406 in these ovarian cancer cells range from 0.05-0.5 µg/mL. Xevinapant exhibits anti-ovarian cancer efficacy both as a single agent and in combination with carboplatin. Xevinapant (30 μg/mL) induced degradation of XIAP in the drug sensitive ovarian cancer cell lines [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Xevinapant (AT-406) is very effective in inhibition of tumor growth in the MDA-MB-231 xenograft model, and has minimal toxicity to animals
[1]
.
Xevinapant is evaluated for its pharmacokinetic (PK) properties in mice, rats, non-human primates and dogs
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model: | SCID mice bearing MDA-MB-231 xenograft tumors [1] |
Dosage: | 30 and 100 mg/kg |
Administration: | p.o.; 5 days a week for 2 weeks |
Result: | Strongly inhibits tumor growth at 30 and 100 mg/kg and completely inhibits tumor growth during the treatment with 100 mg/kg. |
NCT Number | Sponsor | Condition | Start Date | Phase |
---|---|---|---|---|
NCT03871959 | Centre Leon Berard|Merck Sharp & Dohme LLC|Debiopharm International SA |
Adenocarcinoma of the Pancreas|Adenocarcinoma of the Colon|Adenocarcinoma of the Rectum
|
September 15, 2019 | Phase 1 |
NCT03270176 | Debiopharm International SA |
Carcinoma, Non-Small-Cell Lung|Neoplasms
|
October 10, 2017 | Phase 1 |
NCT04122625 | Debiopharm International SA |
Solid Tumor
|
April 8, 2019 | Phase 1|Phase 2 |
NCT04459715 | EMD Serono Research & Development Institute, Inc.|GORTEC (Head and Neck Oncology and Radiotherapy Group)|Merck KGaA, Darmstadt, Germany|EMD Serono |
Squamous Cell Carcinoma of the Head and Neck
|
August 7, 2020 | Phase 3 |
NCT02022098 | Debiopharm International SA |
Squamous Cell Carcinoma of the Head and Neck
|
October 2013 | Not Applicable |
NCT01078649 | Debiopharm International SA |
Cancer|Solid Tumors|Lymphoma|Malignancy
|
March 29, 2010 | Phase 1 |
NCT01265199 | Ascenta Therapeutics|The Leukemia and Lymphoma Society |
Acute Myelogenous Leukemia (AML)
|
February 2011 | Phase 1 |
NCT04962724 | Debiopharm International SA |
Healthy Volunteers
|
August 2, 2021 | Phase 1 |
NCT05519540 | Merck Healthcare KGaA, Darmstadt, Germany, an affiliate of Merck KGaA, Darmstadt, Germany|Merck KGaA, Darmstadt, Germany |
Healthy
|
September 26, 2022 | Phase 1 |
NCT05386550 | EMD Serono Research & Development Institute, Inc.|Merck KGaA, Darmstadt, Germany|EMD Serono |
Head and Neck Cancer
|
October 6, 2022 | Phase 3 |
NCT01930292 | Debiopharm International SA |
Solid Tumors
|
April 2013 | Phase 1 |
Solid
Room temperature in continental US; may vary elsewhere.
Powder | -20°C | 3 years |
---|---|---|
4°C | 2 years | |
In solvent | -80°C | 6 months |
-20°C | 1 month |
DMSO : 100 mg/mL ( 178.03 mM ; Need ultrasonic)
Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
---|
1 mM | 1.7803 mL | 8.9014 mL | 17.8028 mL |
5 mM | 0.3561 mL | 1.7803 mL | 3.5606 mL |
10 mM | 0.1780 mL | 0.8901 mL | 1.7803 mL |
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