|
|
| | 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- Basic information |
| Product 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: | 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 | | CAS: | 2172652-48-9 | | MF: | C20H27ClN6O2S | | MW: | 450.99 | | EINECS: | | | Product Categories: | | | 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- Structure](CAS/20210305/GIF/2172652-48-9.gif) |
| | 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 |
| Boiling point | 663.8±55.0 °C(Predicted) | | density | 1.44±0.1 g/cm3(Predicted) | | solubility | Acetonitrile: Slightly Soluble
DMSO: Soluble
Water: Slightly Soluble | | form | Solid | | pka | 12.31±0.10(Predicted) | | color | Light yellow to yellow |
| | 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- Usage And Synthesis |
| 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.
[4] De Souza, F.I., Zumiotti, A.V., and Da Silva, C.F. Neuregulins 1-α and 1-β on the regeneration the peripheral nerves[J]. Acta Ortop Bras.
[5] J. SMITH. Abstract 1943: 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 1: 1943-1943. DOI: 10.1158/1538-7445.am2020-1943
|
| | 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 |
|