Drug Information
Drug (ID: DG01662) and It's Reported Resistant Information
Name |
RMC-4550
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Synonyms |
RMC-4550; 2172651-73-7; UNII-2Q6NVG4EXB; 2Q6NVG4EXB; CHEMBL4752026; (3-((3S,4S)-4-amino-3-methyl-2-oxa-8-azaspiro[4.5]decan-8-yl)-6-(2,3-dichlorophenyl)-5-methylpyrazin-2-yl)methanol; [3-[(3S,4S)-4-amino-3-methyl-2-oxa-8-azaspiro[4.5]decan-8-yl]-6-(2,3-dichlorophenyl)-5-methylpyrazin-2-yl]methanol; {3-[(3S,4S)-4-amino-3-methyl-2-oxa-8-azaspiro[4.5]decan-8-yl]-6-(2,3-dichlorophenyl)-5-methylpyrazin-2-yl}methanol; 2-Pyrazinemethanol, 3-((3S,4S)-4-amino-3-methyl-2-oxa-8-azaspiro(4.5)dec-8-yl)-6-(2,3-dichlorophenyl)-5-methyl-; 2-Pyrazinemethanol, 3-[(3S,4S)-4-amino-3-methyl-2-oxa-8-azaspiro[4.5]dec-8-yl]-6-(2,3-dichlorophenyl)-5-methyl-; SCHEMBL19785503; RMC-4550 (SHP2 Inhibitor); AMY16974; EX-A3075; XLD65173; BDBM50546219; MFCD31746888; s8718; ZB1559; AKOS037648879; AC-31540; BS-15923; HY-116009; CS-0063450; D70060; A929920; [3-[(3S,4S)-4-AMINO-3-METHYL-2-OXA-8-AZASPIRO[4.5]DECAN-8-YL]-6-(2,3-DICHLOROPHENYL)-5-METHYL-PYRAZIN-2-YL]METHANOL
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Structure | |||||
Drug Resistance Disease(s) |
Disease(s) with Clinically Reported Resistance for This Drug
(2 diseases)
Lung cancer [ICD-11: 2C25]
[1]
Melanoma [ICD-11: 2C30]
[1]
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Target | . | NOUNIPROTAC | [1] | ||
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Formula |
3
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IsoSMILES |
C[C@H]1[C@H](C2(CCN(CC2)C3=NC(=C(N=C3CO)C4=C(C(=CC=C4)Cl)Cl)C)CO1)N
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InChI |
InChI=1S/C21H26Cl2N4O2/c1-12-18(14-4-3-5-15(22)17(14)23)26-16(10-28)20(25-12)27-8-6-21(7-9-27)11-29-13(2)19(21)24/h3-5,13,19,28H,6-11,24H2,1-2H3/t13-,19+/m0/s1
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InChIKey |
IKUYEYLZXGGCRD-ORAYPTAESA-N
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PubChem CID |
Type(s) of Resistant Mechanism of This Drug
UAPP: Unusual Activation of Pro-survival Pathway
Drug Resistance Data Categorized by Their Corresponding Diseases
ICD-02: Benign/in-situ/malignant neoplasm
Colorectal cancer [ICD-11: 2B91]
Drug Sensitivity Data Categorized by Their Corresponding Mechanisms | ||||
Unusual Activation of Pro-survival Pathway (UAPP) | ||||
Key Molecule: Serine/threonine-protein kinase B-raf (BRAF) | [1] | |||
Molecule Alteration | Missense mutation | p.G596R (c.1786G>C) |
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Sensitive Disease | Colorectal cancer [ICD-11: 2B91.1] | |||
Experimental Note | Identified from the Human Clinical Data | |||
Cell Pathway Regulation | RAS/RAF/MEK/ERK signaling pathway | Activation | hsa01521 | |
In Vitro Model | NCI-H358 cells | Lung | Homo sapiens (Human) | CVCL_1559 |
NCI-H508 cells | Colon | Homo sapiens (Human) | CVCL_1564 | |
HEK 293 cells | Kidney | Homo sapiens (Human) | CVCL_0045 | |
Nras cells | N.A. | . | N.A. | |
NCI-H1838 cells | Lung | Homo sapiens (Human) | CVCL_1499 | |
KRAS cells | N.A. | . | N.A. | |
Hras cells | N.A. | . | N.A. | |
In Vivo Model | Athymic Balb/C nude mouse model | Mus musculus | ||
Experiment for Molecule Alteration |
Western blotting analysis | |||
Experiment for Drug Resistance |
Promega assay | |||
Mechanism Description | SHP2 inhibitor treatment decreases oncogenic RAS-RAF-MEK-ERK signaling and cancer growth by disrupting SOS1-mediated RAS-GTP loading. |
Lung cancer [ICD-11: 2C25]
Drug Resistance Data Categorized by Their Corresponding Mechanisms | ||||
Unusual Activation of Pro-survival Pathway (UAPP) | ||||
Key Molecule: Serine/threonine-protein kinase B-raf (BRAF) | [1] | |||
Molecule Alteration | Missense mutation | p.G469A (c.1406G>C) |
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Resistant Disease | Lung adenocarcinoma [ICD-11: 2C25.0] | |||
Experimental Note | Identified from the Human Clinical Data | |||
Cell Pathway Regulation | RAS/RAF/MEK/ERK signaling pathway | Activation | hsa01521 | |
In Vitro Model | NCI-H358 cells | Lung | Homo sapiens (Human) | CVCL_1559 |
NCI-H508 cells | Colon | Homo sapiens (Human) | CVCL_1564 | |
HEK 293 cells | Kidney | Homo sapiens (Human) | CVCL_0045 | |
Nras cells | N.A. | . | N.A. | |
NCI-H1838 cells | Lung | Homo sapiens (Human) | CVCL_1499 | |
KRAS cells | N.A. | . | N.A. | |
Hras cells | N.A. | . | N.A. | |
In Vivo Model | Athymic Balb/C nude mouse model | Mus musculus | ||
Experiment for Molecule Alteration |
Western blotting analysis | |||
Experiment for Drug Resistance |
Promega assay | |||
Mechanism Description | SHP2 inhibitor treatment decreases oncogenic RAS-RAF-MEK-ERK signaling and cancer growth by disrupting SOS1-mediated RAS-GTP loading. |
Drug Sensitivity Data Categorized by Their Corresponding Mechanisms | ||||
Unusual Activation of Pro-survival Pathway (UAPP) | ||||
Key Molecule: Serine/threonine-protein kinase B-raf (BRAF) | [1] | |||
Molecule Alteration | Missense mutation | p.G466V (c.1397G>T) |
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Sensitive Disease | Lung adenocarcinoma [ICD-11: 2C25.0] | |||
Experimental Note | Identified from the Human Clinical Data | |||
Cell Pathway Regulation | RAS/RAF/MEK/ERK signaling pathway | Activation | hsa01521 | |
In Vitro Model | NCI-H358 cells | Lung | Homo sapiens (Human) | CVCL_1559 |
NCI-H508 cells | Colon | Homo sapiens (Human) | CVCL_1564 | |
HEK 293 cells | Kidney | Homo sapiens (Human) | CVCL_0045 | |
Nras cells | N.A. | . | N.A. | |
NCI-H1838 cells | Lung | Homo sapiens (Human) | CVCL_1499 | |
KRAS cells | N.A. | . | N.A. | |
Hras cells | N.A. | . | N.A. | |
In Vivo Model | Athymic Balb/C nude mouse model | Mus musculus | ||
Experiment for Molecule Alteration |
Western blotting analysis | |||
Experiment for Drug Resistance |
Promega assay | |||
Mechanism Description | SHP2 inhibitor treatment decreases oncogenic RAS-RAF-MEK-ERK signaling and cancer growth by disrupting SOS1-mediated RAS-GTP loading. | |||
Key Molecule: Serine/threonine-protein kinase B-raf (BRAF) | [1] | |||
Molecule Alteration | Missense mutation | p.N581D (c.1741A>G) |
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Sensitive Disease | Lung adenocarcinoma [ICD-11: 2C25.0] | |||
Experimental Note | Identified from the Human Clinical Data | |||
Cell Pathway Regulation | RAS/RAF/MEK/ERK signaling pathway | Activation | hsa01521 | |
In Vitro Model | NCI-H358 cells | Lung | Homo sapiens (Human) | CVCL_1559 |
NCI-H508 cells | Colon | Homo sapiens (Human) | CVCL_1564 | |
HEK 293 cells | Kidney | Homo sapiens (Human) | CVCL_0045 | |
Nras cells | N.A. | . | N.A. | |
NCI-H1838 cells | Lung | Homo sapiens (Human) | CVCL_1499 | |
KRAS cells | N.A. | . | N.A. | |
Hras cells | N.A. | . | N.A. | |
In Vivo Model | Athymic Balb/C nude mouse model | Mus musculus | ||
Experiment for Molecule Alteration |
Western blotting analysis | |||
Experiment for Drug Resistance |
Promega assay | |||
Mechanism Description | SHP2 inhibitor treatment decreases oncogenic RAS-RAF-MEK-ERK signaling and cancer growth by disrupting SOS1-mediated RAS-GTP loading. | |||
Key Molecule: Serine/threonine-protein kinase B-raf (BRAF) | [1] | |||
Molecule Alteration | Missense mutation | p.D594N (c.1780G>A) |
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Sensitive Disease | Lung adenocarcinoma [ICD-11: 2C25.0] | |||
Experimental Note | Identified from the Human Clinical Data | |||
Cell Pathway Regulation | RAS/RAF/MEK/ERK signaling pathway | Activation | hsa01521 | |
In Vitro Model | NCI-H358 cells | Lung | Homo sapiens (Human) | CVCL_1559 |
NCI-H508 cells | Colon | Homo sapiens (Human) | CVCL_1564 | |
HEK 293 cells | Kidney | Homo sapiens (Human) | CVCL_0045 | |
Nras cells | N.A. | . | N.A. | |
NCI-H1838 cells | Lung | Homo sapiens (Human) | CVCL_1499 | |
KRAS cells | N.A. | . | N.A. | |
Hras cells | N.A. | . | N.A. | |
In Vivo Model | Athymic Balb/C nude mouse model | Mus musculus | ||
Experiment for Molecule Alteration |
Western blotting analysis | |||
Experiment for Drug Resistance |
Promega assay | |||
Mechanism Description | SHP2 inhibitor treatment decreases oncogenic RAS-RAF-MEK-ERK signaling and cancer growth by disrupting SOS1-mediated RAS-GTP loading. |
Melanoma [ICD-11: 2C30]
Drug Resistance Data Categorized by Their Corresponding Mechanisms | ||||
Unusual Activation of Pro-survival Pathway (UAPP) | ||||
Key Molecule: Serine/threonine-protein kinase B-raf (BRAF) | [1] | |||
Molecule Alteration | Missense mutation | p.V600E (c.1799T>A) |
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Resistant Disease | Melanoma [ICD-11: 2C30.0] | |||
Experimental Note | Identified from the Human Clinical Data | |||
Cell Pathway Regulation | RAS/RAF/MEK/ERK signaling pathway | Activation | hsa01521 | |
In Vitro Model | NCI-H358 cells | Lung | Homo sapiens (Human) | CVCL_1559 |
NCI-H508 cells | Colon | Homo sapiens (Human) | CVCL_1564 | |
HEK 293 cells | Kidney | Homo sapiens (Human) | CVCL_0045 | |
Nras cells | N.A. | . | N.A. | |
NCI-H1838 cells | Lung | Homo sapiens (Human) | CVCL_1499 | |
KRAS cells | N.A. | . | N.A. | |
Hras cells | N.A. | . | N.A. | |
In Vivo Model | Athymic Balb/C nude mouse model | Mus musculus | ||
Experiment for Molecule Alteration |
Western blotting analysis | |||
Experiment for Drug Resistance |
Promega assay | |||
Mechanism Description | SHP2 inhibitor treatment decreases oncogenic RAS-RAF-MEK-ERK signaling and cancer growth by disrupting SOS1-mediated RAS-GTP loading. |
References
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