| Identification | Back Directory | [Name]
G-202 | [CAS]
1245732-48-2 | [Synonyms]
G-202
Zoliflodacin
G202/Zoliflodacin
UPYNTAIBQVNPIH-ODMLWHIESA-N
L-Glutamic acid, N-[12-[[(3S,3aR,4S,6S,6aR,7S,8S,9bS)-6-(acetyloxy)-2,3,3a,4,5,6,6a,7,8,9b-decahydro-3,3a-dihydroxy-3,6,9-trimethyl-8-[[(2Z)-2-methyl-1-oxo-2-buten-1-yl]oxy]-2-oxo-7-[(1-oxooctyl)oxy]azuleno[4,5-b]furan-4-yl]oxy]-12-oxododecyl]-L-asparaginyl-L-γ-glutamyl-L-γ-glutamyl-L-γ-glutamyl- | [Molecular Formula]
C66H100N6O27 | [MDL Number]
MFCD25976815 | [MOL File]
1245732-48-2.mol | [Molecular Weight]
1409.52 |
| Chemical Properties | Back Directory | [Melting point ]
>205°C (dec.) | [storage temp. ]
-20°C Freezer, Under inert atmosphere | [solubility ]
DMSO (Slightly), Methanol (Slightly, Heated, Sonicated) | [form ]
Solid | [color ]
White to Pale Yellow | [Sequence]
Asp-{Ggu}-{Ggu}-{Ggu}-{Ggu} |
| Hazard Information | Back Directory | [Uses]
Zoliflodacin, is a spiropyrimidinetrione bacterial DNA gyrase/topoisomerase inhibitor, and has in vitro antibacterial activity against Gram-positive and Gram-negative organisms, including S. aureus. | [in vivo]
Mipsagargin (G-202; 56 mg/kg; 2 daily; 49 days) alone is able to produce significant (>50%) tumor regression. This regression is stabilized when combined with daily dosing with the oral HDAC4 inhibitor, Tasquinimod (HY-10528)[1].
Mipsagargin (56 mg/kg/day; for 3 consecutive days) produces ～50% average regression of LNCaP xenografts in intact mice over a 30-day period. Significant antitumor effects are also observed against MDA-PCa2b and CWR22R-H out to ≥30 days after a single 3-day course of Mipsagargin[2].
Mipsagargin (67 mg/kg; IV) HaS a half-life of 4.9 hours in BALB/c mice[2].
| Animal Model: | MCF-7 human breast cancers growing in mice[1] | | Dosage: | 56 mg/kg | | Administration: | IV; 2 daily; 49 days | | Result: | Alone was able to produce significant (>50%) tumor regression.
This regression was stabilized when combined with daily dosing with the oral HDAC4 inhibitor, Tasquinimod (10 mg/kg/d; oral).
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| Animal Model: | BALB/c mice[2] | | Dosage: | 67 mg/kg (Pharmacokinetic Analysis) | | Administration: | IV; a single dose | | Result: | Had a half-life of 4.9 hours.
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| [IC 50]
Traditional Cytotoxic Agents |
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