Drug Information
Drug (ID: DG01506) and It's Reported Resistant Information
Name |
E6201
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Synonyms |
E6201; UNII-CZP9GB25HO; E-6201; CZP9GB25HO; E 6201; 603987-35-5; ER-806201; (3S,4R,5Z,8S,9S,11E)-14-(ethylamino)-8,9,16-trihydroxy-3,4-dimethyl-3,4,9,10-tetrahydro-1H-benzo[c][1]oxacyclotetradecine-1,7(8H)-dione; (4~{S},5~{R},6~{Z},9~{S},10~{S},12~{E})-16-(ethylamino)-4,5-dimethyl-9,10,18-tris(oxidanyl)-3-oxabicyclo[12.4.0]octadeca-1(14),6,12,15,17-pentaene-2,8-dione; GTPL7836; SCHEMBL6983345; CHEMBL1097999; BDBM50515043; ZINC34374629; DB11687; (3S,4R,5Z,8S,9S,11E)-14-(Ethylamino)-8, 9,16-trihydroxy-3,4-dimethyl-3,4,9,19-tetrahydro-1H-2-benzoxacyclotetradecine-1,7(8H)-dione; HY-15496; CS-0006796; J-504641; Q27077143; (4S,5R,6Z,9S,10S,12E)-16-(ethylamino)-9,10,18-trihydroxy-4,5-dimethyl-3-oxabicyclo[12.4.0]octadeca-1(14),6,12,15,17-pentaene-2,8-dione; (4S,5R,6Z,9S,10S,12E)-16-ethylamino-9,10,18-trihydroxy-4,5-dimethyl-3-oxabicyclo[12.4.0]octadeca-1(14),6,12,15,17-pentaene-2,8-dione; 1H-2-Benzoxacyclotetradecin-1,7(8H)-dione, 14-(ethylamino)-3,4,9,10-tetrahydro-8,9,16-trihydroxy-3,4-dimethyl-, (3S,4R,5Z,8S,9S,11E)-; 1H-2-Benzoxacyclotetradecin-1,7(8H)-dione, 14-(ethylamino)-3,4,9,10-tetrahydro-8,9,16-trihydroxy-3,4-dimethyl-, (3S,4R,5Z,8S,9S,11E) -
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Indication |
In total 4 Indication(s)
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Structure | |||||
Target | ERK activator kinase 1 (MEK1) | MP2K1_HUMAN | [2] | ||
ERK activator kinase 2 (MEK2) | MP2K2_HUMAN | [2] | |||
MAPK/ERK kinase kinase (MAP3K) | NOUNIPROTAC | [2] | |||
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Formula |
2
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IsoSMILES |
CCNC1=CC\\2=C(C(=C1)O)C(=O)O[C@H]([C@@H](/C=C\\C(=O)[C@H]([C@H](C/C=C2)O)O)C)C
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InChI |
InChI=1S/C21H27NO6/c1-4-22-15-10-14-6-5-7-16(23)20(26)17(24)9-8-12(2)13(3)28-21(27)19(14)18(25)11-15/h5-6,8-13,16,20,22-23,25-26H,4,7H2,1-3H3/b6-5+,9-8-/t12-,13+,16+,20+/m1/s1
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InChIKey |
MWUFVYLAWAXDHQ-HMNLTAHHSA-N
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PubChem CID | |||||
TTD Drug ID |
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
Acute myeloid leukemia [ICD-11: 2A60]
Drug Sensitivity Data Categorized by Their Corresponding Mechanisms | ||||
Unusual Activation of Pro-survival Pathway (UAPP) | ||||
Key Molecule: Receptor-type tyrosine-protein kinase FLT3 (FLT3) | [1] | |||
Molecule Alteration | Missense mutation | p.D835Y (c.2503G>T) |
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Sensitive Disease | Acute myeloid leukemia [ICD-11: 2A60.0] | |||
Experimental Note | Revealed Based on the Cell Line Data | |||
Cell Pathway Regulation | MEK/ERK signaling pathway | Inhibition | hsa04011 | |
In Vitro Model | Ba/F3 cells | Colon | Homo sapiens (Human) | CVCL_0161 |
Ba/F3 cells | Colon | Homo sapiens (Human) | CVCL_0161 | |
Ba/F3 cells | Colon | Homo sapiens (Human) | CVCL_0161 | |
Ba/F3 cells | Colon | Homo sapiens (Human) | CVCL_0161 | |
In Vivo Model | NOG mouse | Mus musculus | ||
Experiment for Molecule Alteration |
Immunoblotting analysis | |||
Experiment for Drug Resistance |
Trypan blue dye exclusion method assay; FACS assay | |||
Mechanism Description | E6201 exerts marked anti-leukemia effects in AML cells and activation of MEK/ERK signaling pathway by NRAS mutation sensitizes E6201-induced pro-apoptotic effects in AML cells. | |||
Key Molecule: Receptor-type tyrosine-protein kinase FLT3 (FLT3) | [1] | |||
Molecule Alteration | Missense mutation | p.D835G (c.2504A>G) |
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Sensitive Disease | Acute myeloid leukemia [ICD-11: 2A60.0] | |||
Experimental Note | Revealed Based on the Cell Line Data | |||
Cell Pathway Regulation | MEK/ERK signaling pathway | Inhibition | hsa04011 | |
In Vitro Model | Ba/F3 cells | Colon | Homo sapiens (Human) | CVCL_0161 |
Ba/F3 cells | Colon | Homo sapiens (Human) | CVCL_0161 | |
Ba/F3 cells | Colon | Homo sapiens (Human) | CVCL_0161 | |
Ba/F3 cells | Colon | Homo sapiens (Human) | CVCL_0161 | |
In Vivo Model | NOG mouse | Mus musculus | ||
Experiment for Molecule Alteration |
Immunoblotting analysis | |||
Experiment for Drug Resistance |
Trypan blue dye exclusion method assay; FACS assay | |||
Mechanism Description | E6201 exerts marked anti-leukemia effects in AML cells and activation of MEK/ERK signaling pathway by NRAS mutation sensitizes E6201-induced pro-apoptotic effects in AML cells. |
Acute lymphocytic leukemia [ICD-11: 2B33]
Drug Sensitivity Data Categorized by Their Corresponding Mechanisms | ||||
Unusual Activation of Pro-survival Pathway (UAPP) | ||||
Key Molecule: Receptor-type tyrosine-protein kinase FLT3 (FLT3) | [1] | |||
Molecule Alteration | Missense mutation | p.D835G (c.2504A>G) |
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Sensitive Disease | Acute lymphocytic leukemia [ICD-11: 2B33.0] | |||
Experimental Note | Revealed Based on the Cell Line Data | |||
Cell Pathway Regulation | MEK/ERK signaling pathway | Inhibition | hsa04011 | |
In Vitro Model | Ba/F3 cells | Colon | Homo sapiens (Human) | CVCL_0161 |
Ba/F3 cells | Colon | Homo sapiens (Human) | CVCL_0161 | |
Ba/F3 cells | Colon | Homo sapiens (Human) | CVCL_0161 | |
Ba/F3 cells | Colon | Homo sapiens (Human) | CVCL_0161 | |
In Vivo Model | NOG mouse | Mus musculus | ||
Experiment for Molecule Alteration |
Immunoblotting analysis | |||
Experiment for Drug Resistance |
Trypan blue dye exclusion method assay; FACS assay | |||
Mechanism Description | E6201 exerts marked anti-leukemia effects in AML cells and activation of MEK/ERK signaling pathway by NRAS mutation sensitizes E6201-induced pro-apoptotic effects in AML cells. | |||
Key Molecule: Receptor-type tyrosine-protein kinase FLT3 (FLT3) | [1] | |||
Molecule Alteration | Missense mutation | p.D835Y (c.2503G>T) |
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Sensitive Disease | Acute lymphocytic leukemia [ICD-11: 2B33.0] | |||
Experimental Note | Revealed Based on the Cell Line Data | |||
Cell Pathway Regulation | MEK/ERK signaling pathway | Inhibition | hsa04011 | |
In Vitro Model | Ba/F3 cells | Colon | Homo sapiens (Human) | CVCL_0161 |
Ba/F3 cells | Colon | Homo sapiens (Human) | CVCL_0161 | |
Ba/F3 cells | Colon | Homo sapiens (Human) | CVCL_0161 | |
Ba/F3 cells | Colon | Homo sapiens (Human) | CVCL_0161 | |
In Vivo Model | NOG mouse | Mus musculus | ||
Experiment for Molecule Alteration |
Immunoblotting analysis | |||
Experiment for Drug Resistance |
Trypan blue dye exclusion method assay; FACS assay | |||
Mechanism Description | E6201 exerts marked anti-leukemia effects in AML cells and activation of MEK/ERK signaling pathway by NRAS mutation sensitizes E6201-induced pro-apoptotic effects in AML cells. |
Melanoma [ICD-11: 2C30]
Drug Sensitivity Data Categorized by Their Corresponding Mechanisms | ||||
Unusual Activation of Pro-survival Pathway (UAPP) | ||||
Key Molecule: Serine/threonine-protein kinase B-raf (BRAF) | [2] | |||
Molecule Alteration | Missense mutation | p.V600E (c.1799T>A) |
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Sensitive Disease | Melanoma [ICD-11: 2C30.0] | |||
Experimental Note | Revealed Based on the Cell Line Data | |||
In Vitro Model | A375 cells | Skin | Homo sapiens (Human) | CVCL_0132 |
G-361 cells | Skin | Homo sapiens (Human) | CVCL_1220 | |
MDA-MB-435s cells | Breast | Homo sapiens (Human) | CVCL_0622 | |
SEKI cells | Skin | Homo sapiens (Human) | CVCL_3162 | |
HMV-1 cells | Uterus | Homo sapiens (Human) | CVCL_8233 | |
HMCB cells | Skin | Homo sapiens (Human) | CVCL_3317 | |
CHL-1 cells | Pleural effusion | Homo sapiens (Human) | CVCL_1122 | |
Experiment for Molecule Alteration |
Western blotting analysis; Immunohistochemistry assay | |||
Experiment for Drug Resistance |
WST-8 assay |
References
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