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Formula | C39H37ClF4N6O6S |
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Molecular Weight | 829.26 | CAS No. | 1799633-27-4 | |
Solubility (25°C)* | In vitro | DMSO | 100 mg/mL (120.58 mM) | |
Ethanol | 100 mg/mL (120.58 mM) | |||
Water | ˂1 mg/mL | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
Description | S63845 is a new, selective MCL-1 inhibitor with the Kd value of 0.19 nM and has no discernible binding to the other BCL-2 members, BCL-2 or BCL-XL. | ||
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In vitro | S63845 induces death of cancer cell lines with known reliance on MCL-1, displaying classical hallmarks of apoptosis that are dependent on caspases and BAX/BAK-mediated mitochondrial outer membrane permeabilisation. It has a 6 fold higher affinity for human MCL-1 over mouse MCL-1[1]. S63845 is effective against haematological cancer-derived cell lines in vitro and in vivo and also AML samples, but does not readily kill normal human haematopoietic progenitor cells[2]. | ||
In vivo | In vivo, S63845 shows potent anti-tumour activity with an acceptable safety margin as a single agent in several cancers. S63845 is well tolerated by the mice with no significant weight loss observed. Some of solid tumour models shows sensitivity to S63845 monotherapy, while many others are only killed when treated with a combination of S63845 and inhibitors of oncogenic kinases[2]. |
Cell Assay: |
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Animal Study: |
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Acute suppression of mitochondrial ATP production prevents apoptosis and provides an essential signal for NLRP3 inflammasome activation [ Immunity, 2024, S1074-7613(24)00492-8] | PubMed: 39571574 |
Fatty acid synthase (FASN) is a tumor-cell-intrinsic metabolic checkpoint restricting T-cell immunity [ Cell Death Discov, 2024, 10(1):417] | PubMed: 39349429 |
Initial AXL and MCL-1 inhibition contributes to abolishing lazertinib tolerance in EGFR-mutant lung cancer cells [ Cancer Sci, 2024, 10.1111/cas.16292] | PubMed: 39039802 |
Defining a Water-Soluble Formulation of Arachidonic Acid as a Novel Ferroptosis Inducer in Cancer Cells [ Biomolecules, 2024, 14(5)555] | PubMed: 38785962 |
Novel markers of MCL1 inhibitor sensitivity in triple-negative breast cancer cells [ J Biol Chem, 2024, 300(6):107375] | PubMed: 38762181 |
Osteosarcoma cells depend on MCL-1 for survival, and osteosarcoma metastases respond to MCL-1 antagonism plus regorafenib in vivo [ BMC Cancer, 2024, 24(1):1350] | PubMed: 39497108 |
Treatment with siRNAs is commonly associated with GPX4 up-regulation and target knockdown-independent sensitization to ferroptosis [ Sci Adv, 2024, 10(11):eadk7329] | PubMed: 38489367 |
Gravitational and mechanical forces drive mitochondrial translation [ bioRxiv, 2024, 10.1101/2023.01.18.524628] | PubMed: none |
Executioner caspases restrict mitochondrial RNA-driven Type I IFN induction during chemotherapy-induced apoptosis [ Nat Commun, 2023, 14(1):1399] | PubMed: 36918588 |
Executioner caspases restrict mitochondrial RNA-driven Type I IFN induction during chemotherapy-induced apoptosis [ Nat Commun, 2023, 14(1):1399] | PubMed: 36918588 |
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.