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Chemical Structure : M4344
CAS No.: 1613191-99-3
Catalog No.: PC-72163Not For Human Use, Lab Use Only.
M4344 (VX-803, Gartisertib) is a highly potent, selective ATR inhibitor with Ki<0.15 nM.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $188 | In stock | |
| 10 mg | $298 | In stock | |
| 25 mg | $478 | In stock | |
| 50 mg | Get quote | ||
| 100 mg | Get quote |
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M4344 (VX-803, Gartisertib) is a highly potent, selective ATR inhibitor with Ki<0.15 nM.
M4344 (VX-803, Gartisertib) showed minimal inhibitory activity against unrelated kinases, with >100-fold selectivity for ATR over 308/312 kinases tested.
M4344 suppressed cancer cell proliferation at lower concentrations, similarly to BAY1895344 and was more potent than berzosertib (VX-970, M6620), ceralasertib, and VE-821.
M4344 (25 nM) strongly suppressed cell viability of prostate DU145 cancer cells in combination of CPT at nanomolar concentrations, M4344 (10 nM) blocked CPT-induced activation of CHK1, a main downstream effector of ATR.
M4344 kills cancer cells under replication stress (RepStress) and with NE genomic signatures by replication-mediated DNA damage.
M4344 synergizes with clinical TOP1 inhibitor (Exatecan), as well as a broad range of widely used clinical agents including etoposide, gemcitabine, cisplatin, and talazoparib.
M4344 is active in patient-derived tumor organoids and xenograft models.
| M.Wt | 541.564 | |
| Formula | C25H29F2N9O3 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO (5.4 mg/mL) |
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| Chemical Name/SMILES |
2-amino-6-fluoro-N-(5-fluoro-4-(4-(4-(oxetan-3-yl)piperazine-1-carbonyl)piperidin-1-yl)pyridin-3-yl)pyrazolo[1,5-a]pyrimidine-3-carboxamide |
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1. Ukhyun Jo, et al. Mol Cancer Ther. 2021 Aug;20(8):1431-1441.
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