AZD5991
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Cat.No：IA2500 Solarbio
CAS：2143010-83-5
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：Solid
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> Small Molecule Compounds > Inhibitors & Antagonists & Agonists > Apoptosis > AZD5991
Product Information
| CAS | 2143010-83-5 |
| Name | AZD5991 |
| Molecular Formula | C35H34ClN5O3S2 |
| Molecular Weight | 672.26 |
| Solubility | Soluble in DMSO |
| Purity | ≥98% |
| Appearance | Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| SMILES | O=C(O)C1=C(CCCOC2=C(C=CC=C3)C3=CC4=C2)C5=C(N1C)C(C6=C(C)N(C)N=C6CSCC7=NN(C)C(CS4)=C7)=C(Cl)C=C5 |
| Target Point | Mcl-1 |
| Passage | Apoptosis |
| Background | AZD5991 is an MCL-1 inhibitor. |
| Biological Activity | AZD5991是MCL-1抑制剂，Ki值为0.13 nM。AZD5991对小鼠源Mcl-1的结合亲和力比对人源Mcl-1低25倍，而之比对大鼠源Mcl-1的亲和力低4倍。[1-3] |
| In Vitro | AZD5991是有效的Mcl-1抑制剂，具有高选择性。AZD5991可与Mcl-1直接结合，通过激活依赖于Bak的线粒体凋亡途径快速诱导癌细胞凋亡，对骨髓瘤和急性髓系白血病效果尤为显著(GI50 < 100nM)。在一系列血液肿瘤和实体瘤来源的细胞系中，AZD5991有倾向性地杀死血液细胞[1][3]。 |
| In Vivo | 在几种多发性骨髓瘤和急性髓性白血病模型中，无论是单次耐受剂量给药或是与bortezomib/venetoclax组合给药，AZD5991都具有有效的抗肿瘤活性，能引起完全的肿瘤消退。在这些体内试验中，AZD5991的细胞毒性活性与其诱导线粒体凋亡途径相关[1]。 |
| Cell Experiment | Animal Models: 皮下接种了MOLP-8细胞的肿瘤模型(接种于雌性C.B.-17 SCID小鼠); Dosages: 10-100 mg/kg; Administration: IV[1] |
| Animal Experiment | 用0-500 nM AZD5991或DMSO处理MOLP-8细胞30分钟。然后将细胞离心，将沉淀物重悬于预冷的lysis buffer中，在冰上孵育20分钟，每5分钟涡流一次。然后将样品拿去离心，测定蛋白浓度。[1] |
| Data Literature Source | [1] Tron AE，et al. Nat Commun. 2018，9(1):5341. [2] Garner TP，et al. Curr Opin Chem Biol. 2017，39:133-142. [3] Adriana E. Tron，et al. AACR Cancer Res. 2018，78(13 Suppl):Abstract nr 302. |
| Unit | Bottle |
| Specification | 1mg |
AZD5991是MCL-1抑制剂。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
Note：
1. The products are all for scientific research use only. Do not use it for medical, clinical diagnosis or treatment, food and cosmetics, etc. Do not store them in ordinary residential areas.
2. For your safety and health, please wear laboratory clothes, disposable gloves and masks.
3. The experimental results may be affected by many factors, after-sale service is limited to the product itself and does not involve other compensation.
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