| Identification | Back Directory | [Name]
2-Pyrazinemethanol, 6-[(2-amino-3-chloro-4-pyridinyl)thio]-3-[(3S,4S)-4-amino-3-methyl-2-oxa-8-azaspiro[4.5]dec-8-yl]-5-methyl- | [CAS]
2172652-48-9 | [Synonyms]
RMC-4630
SHP2-IN-7
Vociprotafib
RMC4630,Phosphatase,RMC 4630,Inhibitor,inhibit
2-Pyrazinemethanol, 6-[(2-amino-3-chloro-4-pyridinyl)thio]-3-[(3S,4S)-4-amino-3-methyl-2-oxa-8-azaspiro[4.5]dec-8-yl]-5-methyl-
(6-((2-Amino-3-chloropyridin-4-yl)thio)-3-((3S,4S)-4-amino-3-methyl-2-oxa-8-azaspiro[4.5]decan-8-yl)-5-methylpyrazin-2-yl)methanol
6-[(2-amino-3-chloro-4-pyridyl)sulfanyl]-3-[(3S,4S)-4-amino-3-methyl-2-oxa-8-azaspiro[4.5]decan-8-yl]-5-methyl-pyrazin-2-yl]methanol | [Molecular Formula]
C20H27ClN6O2S | [MOL File]
2172652-48-9.mol | [Molecular Weight]
450.99 |
| Chemical Properties | Back Directory | [Boiling point ]
663.8±55.0 °C(Predicted) | [density ]
1.44±0.1 g/cm3(Predicted) | [form ]
Solid | [pka]
12.31±0.10(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
Vociprotafib (RMC-4630) is an orally active, selective and potent phosphatase SHP2 inhibitor, which blocks activation of the RAS-RAF-MEK-ERK signaling pathway with antitumor activity. Vociprotafib accelerates the time to, and increases the magnitude of, tumor regressions in Osimertinib (HY-15772)-sensitive EGFR-mutant tumors of mice[1][2][3]. | [in vivo]
Vociprotafib delays and/or reduces tumor regrowth in mice upon cessation of treatment[3].
Vociprotafib is effective at inhibiting tumor growth in a PDX model that has become resistant to Osimertinib via amplification of c-MET[3].
| [References]
[1] WO2018013597
[2] Ou S I, et al. A12 the SHP2 inhibitor RMC-4630 in patients with KRAS-mutant non-small cell lung cancer: preliminary evaluation of a first-in-man phase 1 clinical trial[J]. Journal of Thoracic Oncology, 2020, 15(2): S15-S16.
[3] Smith J A, et al. SHP2 inhibition as the backbone of targeted therapy combinations for the treatment of cancers driven by oncogenic mutations in the RAS pathway[J]. Cancer Research, 2020, 80(16_Supplement): 1943-1943. |
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