Mcl-1 inhibitor 6
Modify Date: 2024-01-02 10:43:56
Mcl-1 inhibitor 6 structure
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Common Name | Mcl-1 inhibitor 6 | ||
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| CAS Number | 2598978-56-2 | Molecular Weight | 518.02 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C26H28ClNO6S | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of Mcl-1 inhibitor 6Mcl-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[1]. |
| Name | Mcl-1 inhibitor 6 |
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| Description | 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[1]. |
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| Related Catalog | |
| Target |
Mcl-1:0.23 nM (Kd) Mcl-1:0.02 μM (Ki) Bcl-2:>10 μM (Kd) Bcl2A1:>10 μM (Kd) Bcl-xL:>10 μM (Kd) Bcl-W:>10 μM (Kd) Bcl-2:10 μM (Ki) Bfl-1:1.57 μM (Ki) |
| In Vitro | 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]. Apoptosis Analysis[1] Cell Line: H929 cells Concentration: 1, 5 μM Incubation Time: For 48 hours Result: Significantly induced apoptosis in a concentration-dependent manner. Western Blot Analysis[1] Cell Line: H929 cells Concentration: 0.1, 0.5, 1, 5 μM Incubation Time: For 4 hours Result: Remarkably upregulated PARP cleavage in H929 cells in a concentration-dependent manner. |
| In Vivo | Mcl-1 inhibitor 6 (compound 40; 60 mg/kg with PO or 20 mg/kg with IP; every two days for 14 days) shows desired in vivo tumor growth inhibition activity[1]. 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]. Animal Model: Balb/c nude female mice (7 weeks) loaded with MV4-11 xenografts[1] Dosage: 60 mg/kg (PO) or 20 mg/kg (IP) Administration: IP or PO; every two days for 14 days Result: Showed desired in vivo tumor growth inhibition activity (T/C = 37.30% and 5.52% by po and ip administration, respectively). Animal Model: SD rats (200-250 g)[1] Dosage: 3 mg/kg (IV) or 10 mg/kg (PO) (Pharmacokinetic Analysis) Administration: IV or PO 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. |
| References |
| Molecular Formula | C26H28ClNO6S |
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| Molecular Weight | 518.02 |