Mitapivat | Pyruvate kinase activator
NMR (Conforms)
Available Options
| Size: | Price | Quantity | |
|---|---|---|---|
| 5 mg | $80.00 | ||
| 25 mg | $270.00 |
Mitapivat (1260075-17-9) is a potent (AC50 = 29 nM PKR; 37 nM PKM2; 33 nM PKL) allosteric activator of pyruvate kinase.1 In clinical use for the treatment of hemolytic anemia2 and a potential agent for the treatment for ß-thalassemia3 and sickle cell anemia4. Pyruvate kinase M2 regulates the rate-limiting step of glycolysis that shifts glucose metabolism from normal respiratory chain to lactate production in tumor cells and is, thus, an important target in cancer cell metabolism.5
References/Citations:
- Kung et al. (2017), AG-348 enhances pyruvate kinase activity in red blood cells from patients with pyruvate kinase deficiency; Blood, 130 1347
- Rab et al. (2021), AG-348 (mitapivat), an allosteric activator of red blood cell pyruvate kinase, increases enzymatic activity, protein stability, and adenosine triphosphate levels over a broad range of PKLR genotypes; Haematologica, 106 238
- Matte et al. (2021), The pyruvate kinase activator mitapivat reduces hemolysis and improves anemia in a ß-thalassemia mouse model; J. Clin. Invest., 131 e144206
- Rab et al. (2021), Decreased activity and stability of pyruvate kinase in sickle cell disease: a novel target for mitapivat therapy; Blood, 137 2997
- Zahra et al. (2020), Pyruvate Kinase M2 and Cancer: The Role of PKM2 in Promoting Tumorigenesis; Oncol. 10 159
NMR (Conforms)
Safety Data Sheet:
Product Data Sheet:
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee
Mitapivat (1260075-17-9) is a potent (AC50 = 29 nM PKR; 37 nM PKM2; 33 nM PKL) allosteric activator of pyruvate kinase.1 In clinical use for the treatment of hemolytic anemia2 and a potential agent for the treatment for ß-thalassemia3 and sickle cell anemia4. Pyruvate kinase M2 regulates the rate-limiting step of glycolysis that shifts glucose metabolism from normal respiratory chain to lactate production in tumor cells and is, thus, an important target in cancer cell metabolism.5
References/Citations:
- Kung et al. (2017), AG-348 enhances pyruvate kinase activity in red blood cells from patients with pyruvate kinase deficiency; Blood, 130 1347
- Rab et al. (2021), AG-348 (mitapivat), an allosteric activator of red blood cell pyruvate kinase, increases enzymatic activity, protein stability, and adenosine triphosphate levels over a broad range of PKLR genotypes; Haematologica, 106 238
- Matte et al. (2021), The pyruvate kinase activator mitapivat reduces hemolysis and improves anemia in a ß-thalassemia mouse model; J. Clin. Invest., 131 e144206
- Rab et al. (2021), Decreased activity and stability of pyruvate kinase in sickle cell disease: a novel target for mitapivat therapy; Blood, 137 2997
- Zahra et al. (2020), Pyruvate Kinase M2 and Cancer: The Role of PKM2 in Promoting Tumorigenesis; Oncol. 10 159
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1-855-FOCUS21
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