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 No.
- 2172652-48-9
- Chemical 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-
- Synonyms
- RMC-4630;SHP2-IN-7;Vociprotafib;RMC-4630, 10 mM in DMSO;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
- CBNumber:
- CB38755327
- Molecular Formula:
- C20H27ClN6O2S
- Molecular Weight:
- 450.99
- MDL Number:
- MOL File:
- 2172652-48-9.mol
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- Properties
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 |
FDA UNII | C4YBF9170L |
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- Chemical Properties,Uses,Production
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.
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- Preparation Products And Raw materials
Raw materials
Preparation Products
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- Suppliers
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