1799633-27-4
S63845
CAS: 1799633-27-4
Molecular Formula: C39H37ClF4N6O6S
1799633-27-4 - Names and Identifiers
1799633-27-4 - Physico-chemical Properties
| Molecular Formula | C39H37ClF4N6O6S |
| Molar Mass | 829.26 |
| Density | 1.46±0.1 g/cm3(Predicted) |
| Boling Point | 852.6±65.0 °C(Predicted) |
| Solubility | DMSO : 33.33 mg/mL (40.19 mM; Need ultrasonic)H2O : < 0.1 mg/mL (insoluble) |
| pKa | 2.54±0.11(Predicted) |
| Storage Condition | -20℃ |
| Use | S63845 is a potent selective myeloid leukemia 1 (MCL1) inhibitor with a Kd value of 0.19 nM in combination with human MCL1. |
| In vitro study | S63845 induces the death of cancer cell lines by inhibiting MCL-1, so that the cancer cells appear a variety of classical apoptosis markers, such as some apoptosis markers that rely on capsas and BAX/BAK mediated increase of mitochondrial outer membrane permeability. The affinity of S63845 for human MCL-1 was 6-fold higher than that for murine MCL-1. In vitro and in vivo experiments, S63845 is effective against blood cancer-derived cell lines, AML samples, and does not kill normal human blood progenitor cells. |
| In vivo study | In vivo, S63845 has potent anti-tumor activity as a safety guarantee of an acceptable range for monotherapy in several cancers. In mice, S63845 was well tolerated without significant weight loss. Some solid tumor models are sensitive to single-agent administration of S62845, while in others, only when S63845 is administered in combination with an inhibitor of oncogenic kinase, has a killing effect on tumor cells. |
1799633-27-4 - Reference
| Reference Show more | 1: Kotschy A, Szlavik Z, Murray J, Davidson J, Maragno AL, Le Toumelin-Braizat G, Chanrion M, Kelly GL, Gong JN, Moujalled DM, Bruno A, Csekei M, Paczal A, Szabo ZB, Sipos S, Radics G, Proszenyak A, Balint B, Ondi L, Blasko G, Robertson A, Surgenor A, Dokurno P, Chen I, Matassova N, Smith J, Pedder C, Graham C, Studeny A, Lysiak-Auvity G, Girard AM, Gravé F, Segal D, Riffkin CD, Pomilio G, Galbraith LC, Aubrey BJ, Brennan MS, Herold MJ, Chang C, Guasconi G, Cauquil N, Melchiore F, Guigal-Stephan N, Lockhart B, Colland F, Hickman JA, Roberts AW, Huang DC, Wei AH, Strasser A, Lessene G, Geneste O. The MCL1 inhibitor S63845 is tolerable and effective in diverse cancer models. Nature. 2016 Oct 19;538(7626):477-482. doi: 10.1038/nature19830. [Epub ahead of print] PubMed PMID: 27760111. 2: Nagai Y, Ueno S, Saeki Y, Soga F, Yanagihara T. Expression of the D3 dopamine receptor gene and a novel variant transcript generated by alternative splicing inhuman peripheral blood lymphocytes. Biochem Biophys Res Commun. 1993 Jul 15;194(1):368-74. PubMed PMID: 7916609. |
1799633-27-4 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.206 ml | 6.029 ml | 12.059 ml |
| 5 mM | 0.241 ml | 1.206 ml | 2.412 ml |
| 10 mM | 0.121 ml | 0.603 ml | 1.206 ml |
| 5 mM | 0.024 ml | 0.121 ml | 0.241 ml |
Last Update：2024-01-02 23:10:35
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Product Name: S63845 Visit Supplier Webpage Request for quotationCAS: 1799633-27-4
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Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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