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| Replacement Information |
|---|
| Empirical Formula | CAS # |
|---|---|
| C₁₇H₁₆N₄O₂S₂ | 1221186-53-3 |
| 产品目录编号 | 库存情况 | 包装 | 数量 / 包装 | 价格 | 数量 | |
|---|---|---|---|---|---|---|
| 5.05487.0001.1753 |
| 玻璃瓶 | 5 mg |
| — |
| Description | |
|---|---|
| Overview | A cell-permeable thienopyrrolopyridazinone that exhibits good aqueous solubility (29.6 µg/mL or 79.5 µM in PBS, pH 7.4) and acts as a potent allosteric PKM2 activator (AC50 = 92 nM; [PKM2] = 0.1 nM) by stabilizing PKM2 tetramer via stoichiometric interaction with FBP-bound PKM2 (2 activator/4 FBP/tetramer) in a similar manner as PKM2 Activator III (Cat. No. 504537). Reprorted to retard human lung carcinoma H1299 proliferation under hypoxia, but not normoxia, condition in cultures (doubling time = 50 and 35 h, respectively, with or without 30 µM TEPP-46; 1% O2) in vitro and impair H1299 tumorigenesis in mice (50 mg/kg/12 h p.o.) in vivo with no apparent toxicity. |
| Catalogue Number | 505487 |
| Brand Family | Calbiochem® |
| Synonyms | Pyruvate Kinase M2 Activator IV, ML265, NCGC00186528, TEPP46, 6-((3-Aminophenyl)methyl)-4-methyl-2-methylsulfinylthieno[3,4]pyrrolo[1,3-d]pyridazin-5-one |
| References | |
|---|---|
| References | Anastasiou, D., et al. 2012. Nat. Chem. Biol. 8, 839. Jiang, J.K., et al. 2010. Bioorg. Med. Chem. Lett. 20, 3387. |
| Product Information | |
|---|---|
| CAS number | 1221186-53-3 |
| Form | White solid |
| Hill Formula | C₁₇H₁₆N₄O₂S₂ |
| Chemical formula | C₁₇H₁₆N₄O₂S₂ |
| Reversible | Y |
| Structure formula Image | |
| Biological Information | |
|---|---|
| Primary Target | PKM2 |
| Purity | ≥98% by HPLC |
| Physicochemical Information | |
|---|---|
| Cell permeable | Y |
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| Toxicological Information |
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| Safety Information according to GHS |
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| Product Usage Statements |
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| Packaging Information | |
|---|---|
| Packaged under inert gas | Packaged under inert gas |
| Transport Information |
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| Supplemental Information |
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| Specifications |
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