Mcl-1 inhibitor 6
Based on 1 Customer Validation
Mcl-1 inhibitor 6 is an orally active, selective myeloid cell leukemia 1 (Mcl-1) protein inhibitor with a Kd of 0.23 nM and a Ki of 0.02 μM. Mcl-1 inhibitor 6 possesses superior selectivity over other Bcl-2 family members (Bcl-2, Bcl2A1, Bcl-xL, and Bcl-w, Kd>10 μM). Mcl-1 inhibitor 6 is a potent antitumor agent.
For research use only. We do not sell to patients.
- Purity: 98.77%
- CAS No.: 2598978-56-2
- Formula: C26H28ClNO6S
- Molecular Weight:518.02
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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Mcl-1 0.23 nM (Kd) |
Mcl-1 0.02 μM (Ki) |
Bcl-2 >10 μM (Kd) |
Bcl-2 10 μM (Ki) |
Bcl2A1 >10 μM (Kd) |
Bcl-xL >10 μM (Kd) |
Bcl-W >10 μM (Kd) |
Bfl-1 1.57 μM (Ki) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| K562 | IC50 |
>30 μM
Compound: 40
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Antiproliferative activity against human K562 cells assessed as decrease in cell viability measured after 72 hrs by MTT assay
Antiproliferative activity against human K562 cells assessed as decrease in cell viability measured after 72 hrs by MTT assay
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[PMID: 34342996] |
| MV4-11 | IC50 |
0.7 μM
Compound: 40
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Antiproliferative activity against human MV4-11 cells assessed as decrease in cell viability measured after 72 hrs by MTT assay
Antiproliferative activity against human MV4-11 cells assessed as decrease in cell viability measured after 72 hrs by MTT assay
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[PMID: 34342996] |
| NCI-H23 | IC50 |
3.02 μM
Compound: 40
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Antiproliferative activity against human NCI-H23 cells assessed as decrease in cell viability measured after 72 hrs by MTT assay
Antiproliferative activity against human NCI-H23 cells assessed as decrease in cell viability measured after 72 hrs by MTT assay
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[PMID: 34342996] |
| NCI-H929 | IC50 |
0.36 μM
Compound: 40
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Antiproliferative activity against human NCI-H929 cells assessed as decrease in cell viability measured after 72 hrs by MTT assay
Antiproliferative activity against human NCI-H929 cells assessed as decrease in cell viability measured after 72 hrs by MTT assay
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[PMID: 34342996] |
| SK-BR-3 | IC50 |
2.84 μM
Compound: 40
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Antiproliferative activity against human SK-BR-3 cells assessed as decrease in cell viability measured after 72 hrs by MTT assay
Antiproliferative activity against human SK-BR-3 cells assessed as decrease in cell viability measured after 72 hrs by MTT assay
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[PMID: 34342996] |
Mcl-1 inhibitor 6 has Kis of 10 μM and 1.57μM for Bcl-2 and Bfl-1, respectively[1].
Mcl-1 inhibitor 6 (1, 5 μM; for 48 h) significantly induces apoptosis in a concentration-dependent manner[1].
Mcl-1 inhibitor 6 (0.1, 5 μM; for 4 h) remarkably upregulates PARP cleavage in H929 cells in a concentration-dependent manner[1].
Mcl-1 inhibitor 6 (for 72 h) shows antiproliferative activities against the tumor cell lines (H929, MV4-11, SK-BR-3, NCI-H23; IC50=0.36-3.02 μM). Mcl-1 inhibitor 6 shows ideal selectivity against CML cell line K562 (IC50>30 μM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:H929 cells
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Concentration:1, 5 μM
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Incubation Time:For 48 hours
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Result:Significantly induced apoptosis in a concentration-dependent manner.
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Cell Line:H929 cells
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Concentration:0.1, 0.5, 1, 5 μM
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Incubation Time:For 4 hours
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Result:Remarkably upregulated PARP cleavage in H929 cells in a concentration-dependent manner.
Mcl-1 inhibitor 6 (3 mg/kg with IV or 10 mg/kg with PO) has a T1/2 of 2.3 hours, a CL of 15.18 mL/min•kg by IV[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 nude female mice (7 weeks) loaded with MV4-11 xenografts[1]
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Dosage:60 mg/kg (PO) or 20 mg/kg (IP)
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Administration:IP or PO; every two days for 14 days
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Result:Showed desired in vivo tumor growth inhibition activity (T/C = 37.30% and 5.52% by po and ip administration, respectively).
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Animal Model:SD rats (200-250 g)[1]
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Dosage:3 mg/kg (IV) or 10 mg/kg (PO) (Pharmacokinetic Analysis)
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Administration:IV or PO
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Result:Had a T1/2 of 2.3 hours, a CL of 15.18 mL/min•kg by IV.
Had a T1/2 of 2.1 hours, a CL of 36.8 mL/min•kg and a Cmax of 2012.95 ng/mL.
Chemical Information
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CAS No. 2598978-56-2
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Appearance Solid
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Molecular Weight 518.02
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Formula C26H28ClNO6S
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Color White to off-white
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SMILES
O=C(C1=C(C)C(S(=O)(C2=CC=C(C(C)=O)C=C2)=O)=C(C)N1CCCOC3=CC(C)=C(Cl)C(C)=C3)O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (193.04 mM; ultrasonic and warming and heat to 60°C; 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)
Purity & Documentation
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Data Sheet (277 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
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 | 1.9304 mL | 9.6521 mL | 19.3043 mL | 48.2607 mL |
| 5 mM | 0.3861 mL | 1.9304 mL | 3.8609 mL | 9.6521 mL | |
| 10 mM | 0.1930 mL | 0.9652 mL | 1.9304 mL | 4.8261 mL | |
| 15 mM | 0.1287 mL | 0.6435 mL | 1.2870 mL | 3.2174 mL | |
| 20 mM | 0.0965 mL | 0.4826 mL | 0.9652 mL | 2.4130 mL | |
| 25 mM | 0.0772 mL | 0.3861 mL | 0.7722 mL | 1.9304 mL | |
| 30 mM | 0.0643 mL | 0.3217 mL | 0.6435 mL | 1.6087 mL | |
| 40 mM | 0.0483 mL | 0.2413 mL | 0.4826 mL | 1.2065 mL | |
| 50 mM | 0.0386 mL | 0.1930 mL | 0.3861 mL | 0.9652 mL | |
| 60 mM | 0.0322 mL | 0.1609 mL | 0.3217 mL | 0.8043 mL | |
| 80 mM | 0.0241 mL | 0.1207 mL | 0.2413 mL | 0.6033 mL | |
| 100 mM | 0.0193 mL | 0.0965 mL | 0.1930 mL | 0.4826 mL |
Mcl-1 inhibitor 6 Related Classifications
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