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Mcl-1 inhibitor 6

Catalog No.GC66017

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.

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Mcl-1 inhibitor 6 Chemical Structure

Cas No.: 2598978-56-2

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50mg
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Sample solution is provided at 25 µL, 10mM.

Product Documents

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Background

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].

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.

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.

Chemical Properties

Cas No. 2598978-56-2 SDF Download SDF
Formula C26H28ClNO6S M.Wt 518.02
Solubility DMSO : 100 mg/mL (193.04 mM; ultrasonic and warming and heat to 60°C) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 1.9304 mL 9.6521 mL 19.3043 mL
5 mM 0.3861 mL 1.9304 mL 3.8609 mL
10 mM 0.193 mL 0.9652 mL 1.9304 mL
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