MPC-3100
Based on 1 Customer Validation
MPC-3100 is an orally bioavailable, synthetic, second-generation small-molecule inhibitor of Hsp90 with potential antineoplastic activity.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 98.4%
- CAS No.: 958025-66-6
- Formule: C22H25BrN6O4S
- Masse moléculaire:549.44
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Stockage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
Activité biologique
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
0.77 μM
Compound: 28g, MPC-3100
|
Cytotoxicity against human A549 cells assessed as inhibition of tumor growth incubated for 72 hrs by luminometry
Cytotoxicity against human A549 cells assessed as inhibition of tumor growth incubated for 72 hrs by luminometry
|
[PMID: 22913511] |
| BT-474 | IC50 |
0.55 μM
Compound: 28g, MPC-3100
|
Cytotoxicity against human BT474 cells assessed as inhibition of tumor growth incubated for 72 hrs by luminometry
Cytotoxicity against human BT474 cells assessed as inhibition of tumor growth incubated for 72 hrs by luminometry
|
[PMID: 22913511] |
| DU-145 | IC50 |
0.1 μM
Compound: 28g, MPC-3100
|
Inhibition of human HSP90 in DU145 cells assessed as degradation of Akt incubated for 24 hrs by Western blot method
Inhibition of human HSP90 in DU145 cells assessed as degradation of Akt incubated for 24 hrs by Western blot method
|
[PMID: 22913511] |
| DU-145 | IC50 |
0.1 μM
Compound: 28g, MPC-3100
|
Inhibition of human HSP90 in DU145 cells assessed as degradation of Her2 incubated for 24 hrs by Western blot method
Inhibition of human HSP90 in DU145 cells assessed as degradation of Her2 incubated for 24 hrs by Western blot method
|
[PMID: 22913511] |
| DU-145 | IC50 |
0.53 μM
Compound: 28g, MPC-3100
|
Cytotoxicity against human DU145 cells assessed as inhibition of tumor growth incubated for 72 hrs by luminometry
Cytotoxicity against human DU145 cells assessed as inhibition of tumor growth incubated for 72 hrs by luminometry
|
[PMID: 22913511] |
| HCT-116 | IC50 |
0.06 μM
Compound: 28g, MPC-3100
|
Inhibition of human HSP90 in HCT116 cells expressing Her2 gene assessed as degradation of Her2 after 4 hrs by luciferase reporter gene assay
Inhibition of human HSP90 in HCT116 cells expressing Her2 gene assessed as degradation of Her2 after 4 hrs by luciferase reporter gene assay
|
[PMID: 22913511] |
| HCT-116 | IC50 |
0.1 μM
Compound: 28g, MPC-3100
|
Inhibition of human HSP90 in HCT116 cells assessed as degradation of Akt incubated for 24 hrs by Western blot method
Inhibition of human HSP90 in HCT116 cells assessed as degradation of Akt incubated for 24 hrs by Western blot method
|
[PMID: 22913511] |
| HCT-116 | IC50 |
0.1 μM
Compound: 28g, MPC-3100
|
Inhibition of human HSP90 in HCT116 cells assessed as degradation of Her2 incubated for 24 hrs by Western blot method
Inhibition of human HSP90 in HCT116 cells assessed as degradation of Her2 incubated for 24 hrs by Western blot method
|
[PMID: 22913511] |
| HCT-116 | IC50 |
0.54 μM
Compound: 28g, MPC-3100
|
Cytotoxicity against human HCT116 cells assessed as inhibition of tumor growth incubated for 72 hrs by luminometry
Cytotoxicity against human HCT116 cells assessed as inhibition of tumor growth incubated for 72 hrs by luminometry
|
[PMID: 22913511] |
| HT-29 | IC50 |
0.42 μM
Compound: 28g, MPC-3100
|
Cytotoxicity against human HT-29 cells assessed as inhibition of tumor growth incubated for 72 hrs by luminometry
Cytotoxicity against human HT-29 cells assessed as inhibition of tumor growth incubated for 72 hrs by luminometry
|
[PMID: 22913511] |
| LNCaP | IC50 |
0.51 μM
Compound: 28g, MPC-3100
|
Cytotoxicity against human LNCAP cells assessed as inhibition of tumor growth incubated for 72 hrs by luminometry
Cytotoxicity against human LNCAP cells assessed as inhibition of tumor growth incubated for 72 hrs by luminometry
|
[PMID: 22913511] |
| MV4-11 | IC50 |
0.25 μM
Compound: 28g, MPC-3100
|
Cytotoxicity against human MV4-11 cells assessed as inhibition of tumor growth incubated for 72 hrs by luminometry
Cytotoxicity against human MV4-11 cells assessed as inhibition of tumor growth incubated for 72 hrs by luminometry
|
[PMID: 22913511] |
| NCI/ADR-RES | IC50 |
4.3 μM
Compound: 28g, MPC-3100
|
Cytotoxicity against human NCI-ADR-RES cells overexpressing P-gp 1 assessed as inhibition of tumor growth incubated for 72 hrs by luminometry
Cytotoxicity against human NCI-ADR-RES cells overexpressing P-gp 1 assessed as inhibition of tumor growth incubated for 72 hrs by luminometry
|
[PMID: 22913511] |
| NCI-H69 | IC50 |
0.15 μM
Compound: 28g, MPC-3100
|
Cytotoxicity against human NCI-H69 cells assessed as inhibition of tumor growth incubated for 72 hrs by luminometry
Cytotoxicity against human NCI-H69 cells assessed as inhibition of tumor growth incubated for 72 hrs by luminometry
|
[PMID: 22913511] |
| NCI-N87 | IC50 |
0.1 μM
Compound: 28g, MPC-3100
|
Inhibition of human HSP90 in NCI-N87 cells assessed as degradation of Her2 incubated for 24 hrs by Western blot method
Inhibition of human HSP90 in NCI-N87 cells assessed as degradation of Her2 incubated for 24 hrs by Western blot method
|
[PMID: 22913511] |
| NCI-N87 | IC50 |
0.2 μM
Compound: 28g, MPC-3100
|
Cytotoxicity against human NCI-N87 cells assessed as inhibition of tumor growth incubated for 72 hrs by luminometry
Cytotoxicity against human NCI-N87 cells assessed as inhibition of tumor growth incubated for 72 hrs by luminometry
|
[PMID: 22913511] |
| OVCAR-8 | IC50 |
0.49 μM
Compound: 28g, MPC-3100
|
Cytotoxicity against human OVCAR8 cells assessed as inhibition of tumor growth incubated for 72 hrs by luminometry
Cytotoxicity against human OVCAR8 cells assessed as inhibition of tumor growth incubated for 72 hrs by luminometry
|
[PMID: 22913511] |
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 958025-66-6
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Appearance Solid
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Masse moléculaire 549.44
-
Formule C22H25BrN6O4S
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Color White to off-white
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SMILES
NC1=C2C(N(CCC3CCN(C([C@@H](O)C)=O)CC3)C(SC4=C(Br)C=C(OCO5)C5=C4)=N2)=NC=N1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
DMSO : 5.5 mg/mL (10.01 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureté et documentation
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Fiche technique (272 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.8200 mL | 9.1002 mL | 18.2003 mL | 45.5009 mL |
| 5 mM | 0.3640 mL | 1.8200 mL | 3.6401 mL | 9.1002 mL | |
| 10 mM | 0.1820 mL | 0.9100 mL | 1.8200 mL | 4.5501 mL |