ChemicalBook >> CAS DataBase List >>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-

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
Last updated:2025-04-17 18:22:24

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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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- RMC-4630 SHP2-IN-7 Vociprotafib RMC4630,Phosphatase,RMC 4630,Inhibitor,inhibit 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 (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 RMC-4630, 10 mM in DMSO 2172652-48-9