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Mcl-1 inhibitor 6
Mcl-1 inhibitor 6 是一种口服有效的，选择性的骨髓细胞白血病 1 (Mcl-1) 蛋白抑制剂，Kd 值为 0.23 nM，Ki 值为 0.02 μM。Mcl-1 inhibitor 6 对 Mcl-1 的选择性高于其他 Bcl-2 家族成员 (Bcl-2、Bcl2A1、Bcl-xL 和 Bcl-w，Kd>10 μM)。Mcl-1 inhibitor 6 是一种有效的抗肿瘤剂。
Mcl-1 inhibitor 6 Chemical Structure
CAS No. : 2598978-56-2
| 规格 |
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是否有货 |
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| 100 mg |
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询价 |
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| 250 mg |
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询价 |
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| 500 mg |
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询价 |
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* Please select Quantity before adding items.
| 生物活性 |
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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| IC50 & Target[1] |
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Mcl-1
0.23 nM (Kd)
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Mcl-1
0.02 μM (Ki)
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Bcl-2
>10 μM (Kd)
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Bcl2A1
>10 μM (Kd)
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Bcl-xL
>10 μM (Kd)
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Bcl-W
>10 μM (Kd)
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Bcl-2
10 μM (Ki)
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Bfl-1
1.57 μM (Ki)
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体外研究
(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].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
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. |
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体内研究
(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].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
| 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. |
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| 分子量 |
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| Formula |
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| CAS 号 |
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis.
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| 参考文献 |
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[1]. Peng-Ju Zhu, et al. Discovery of 3,5-Dimethyl-4-Sulfonyl-1 H-Pyrrole-Based Myeloid Cell Leukemia 1 Inhibitors with High Affinity, Selectivity, and Oral Bioavailability. J Med Chem. 2021 Aug 12;64(15):11330-11353.
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