Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Hypothemycin is a fungal polyketide and is a multikinase inhibitor (Kis: 10/70 nM, 17/38 nM, 90 nM, 900 nM/1.5 μM, and 8.4/2.4 μM for VEGFR2/VEGFR1, MEK1/MEK2, FLT-3, PDGFRβ/PDGFRα, and ERK1/ERK2, respectively).
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | 35 days | $ 498.00 | |
5 mg | 35 days | $ 2,360.00 |
Description | Hypothemycin is a fungal polyketide and is a multikinase inhibitor (Kis: 10/70 nM, 17/38 nM, 90 nM, 900 nM/1.5 μM, and 8.4/2.4 μM for VEGFR2/VEGFR1, MEK1/MEK2, FLT-3, PDGFRβ/PDGFRα, and ERK1/ERK2, respectively). |
Targets&IC50 | MEK2:38 nM (ki), PDGFRβ:900 nM (ki), PDGFRα:1.5 μM (ki), ERK2:2.4 μM (ki), FLT3:90 nM (ki), MEK1:17 nM (ki), ERK1:8.4 μM (ki), VEGFR1:70 nM (ki), VEGFR2:10 nM (ki) |
In vitro | Hypothemycin demonstrates inhibitory activity against a range of mutated cells: it targets EOL1 eosinophilic cells with FIP1L1-PDGFRα mutations, MV-4-11 acute myeloid leukemia cells with FLT3-ITD mutations, and COLO829 melanoma cells with BRAF V600E mutations, displaying IC50 values of 0.4 nM, 6 nM, and 50 nM, respectively. Additionally, it inhibits HUVEC cells with VEGFR mutations, P815 mastocytoma cells with c-KIT D814Y mutations, A459 non-small cell lung cancer (NSCLC) cells with KRAS mutations, and SKOV-3 ovarian cells with HER2 mutations, with IC50 values of 70 nM, 370 nM, 6.0 μM, and 7.0 μM, respectively. |
In vivo | Hypothemycin (10 mg/kg) kills T. brucei in infected mice. However, it completely curing the infection in one third of animals, although high doses of Hypothemycin (>10 mg/kg) leads to side effects. |
Molecular Weight | 378.37 |
Formula | C19H22O8 |
CAS No. | 76958-67-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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Hypothemycin 76958-67-3 Others inhibitor inhibit