AZD-5991 NEW
| Price | $5 | $4 | $2 |
| Package | 1kg | 10kg | 100kg |
| Min. Order: | 1kg |
| Supply Ability: | 100kg |
| Update Time: | 2025-06-24 |
Product Details
| Product Name: AZD-5991 | CAS No.: 2143061-81-6 |
| Min. Order: 1kg | Purity: 99% |
| Supply Ability: 100kg | Release date: 2025/06/24 |
| Lead time: in stock | Packaging: bag/bottle/drum//IBC, as request |
| Delivery: By sea, by air, by express | Origin: Manufacturer, advantage products |
| COA, MSDS: Available, contact us for details | Contact: Tina |
PRODUCT INFORMATION
| Name | AZD-5991 |
|---|
| Description | AZD-5991 is a potent and selective Mcl-1 inhibitor with an IC50 of 0.7 nM in FRET assay and a Kd of 0.17 nM in surface plasmon resonance (SPR) assay. |
|---|---|
| Related Catalog | Signaling Pathways >> Apoptosis >> Bcl-2 Family Research Areas >> Cancer |
| Target | Mcl-1:0.7 nM (IC50) Mcl-1:0.17 nM (Kd) |
| In Vitro | The selectivity of AZD-5991 is evaluated against pro-survival Bcl-2 family members using FRET assays. AZD-5991 is selective for Mcl-1 (IC50 0.72?nM, Ki=200?pM) vs. Bcl-2 (IC50=20?μM, Ki=6.8?μM), Bcl-xL (IC50=36?μM, Ki=18?μM), Bcl-w (IC50=49?μM, Ki=25?μM), and Bfl-1 (IC50=24?μM, Ki=12?μM). MOLP-8, MV4-11, and NCI-H23 cells are treated with AZD5991 (EC50=0.033, 0.024, 0.19?μM, respectively).AZD5991 binds directly to Mcl-1 and induces rapid apoptosis in cancer cells, most notably myeloma and acute myeloid leukemia, by activating the Bak-dependent mitochondrial apoptotic pathway. AZD5991 reduces the levels of Mcl-1 protein in AZD5991-sensitive but not in AZD5991-resistant MM cell lines further supporting the notion that activation of caspases by AZD5991 reduces Mcl-1 protein levels in AZD5991-sensitive cell lines[1]. |
| In Vivo | A single intravenous (i.v.) dose of AZD5991 leads to a dose-dependent antitumor effect ranging from tumor growth inhibition (TGI) to tumor regression (TR). Ten days after treatment, AZD5991 shows 52% and 93% TGI (p<0.0001) at 10 and 30?mg/kg, respectively. At the same time point, AZD5991 at 60?mg/kg leads to 99% TR with no detectable tumors in 6 out of 7 mice, while complete TR is seen in 7 out of 7 mice in the 100?mg/kg dose group. AZD5991 also shows a dose-dependent duration of response with tumors in the 100?mg/kg group growing back later than those in the 60?mg/kg group. The magnitude of in vivo tumor efficacy is correlated with activation of caspase-3 in the tumor and concentration of AZD5991 in plasma. Treatment with AZD5991 was well tolerated at all dose levels with no significant body weight loss. A single dose of AZD5991 36 days after the first dose causes tumor regression in 4 out of 4 mice. In mice dosed with AZD5991 at 100?mg/kg on day 0 and day 1, tumors grow back later than those dosed with a single dose of AZD5991 at the same dose level[1]. |
| Animal Admin | Mice and Rats[1] In mice, drugs (e.g., AZD5991; 10-100?mg/kg) are dosed intravenously in a volume of 5?mL/kg except for Venetoclax that is dosed orally in a volume of 10?mL/kg. One million MV4-11, five million MOLP-8, ten million NCI-H929 or five million OCI-AML3 cells are injected subcutaneously in the right flank of mice in a volume of 0.1?mL. In rats, AZD5991 (10-100?mg/kg) is dosed intravenously in a volume of 10?mL/kg. Ten million MV4-11 cells are injected subcutaneously in the right flank of rats in a volume of 0.1?mL. Tumor volumes (measured by caliper), animal body weight, and tumor condition are recorded twice weekly for the duration of the study. The tumor volume is calculated[1]. |
| References | [1]. Tron AE, et al. Discovery of Mcl-1-specific inhibitor AZD5991 and preclinical activity in multiple myeloma and acute myeloid leukemia. Nat Commun. 2018 Dec 17;9(1):5341. |
| Molecular Formula | C35H34ClN5O3S2 |
|---|---|
| Molecular Weight | 672.26 |
| Storage condition | 2-8℃ |
Company Profile
Our company is a high-tech enterprise specializing in chemical raw materials such as electronic materials, optoelectronic materials, semiconductor materials, UV monomers, silane catalysts, cosmetic raw materials, etc. The company integrates research and development, production, customized synthesis, and sales, and is committed to providing customers with high-quality chemical product solutions.
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Contact name: Tina
Email address: Tina@fdachem.com
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Company Profile Introduction
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