Drug Information
Drug (ID: DG01628) and It's Reported Resistant Information
Name |
LY3009120
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Synonyms |
LY3009120; 1454682-72-4; LY-3009120; DP-4978; UNII-1GDT36RARO; LY 3009120; 1GDT36RARO; DP 4978; 1-(3,3-dimethylbutyl)-3-[2-fluoro-4-methyl-5-[7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl]phenyl]urea; CHEMBL3577124; 1-(3,3-Dimethylbutyl)-3-{2-Fluoro-4-Methyl-5-[7-Methyl-2-(Methylamino)pyrido[2,3-D]pyrimidin-6-Yl]phenyl}urea; 1-(3,3-Dimethylbutyl)-3-(2-fluoro-4-methyl-5-(7-methyl-2-(methylamino)pyrido(2,3-d)pyrimidin-6-yl)phenyl)urea; N-(3,3-Dimethylbutyl)-N'-[2-fluoro-4-methyl-5-[7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl]phenyl]urea; Urea, N-(3,3-dimethylbutyl)-N'-(2-fluoro-4-methyl-5-(7-methyl-2-(methylamino)pyrido(2,3-d)pyrimidin-6-yl)phenyl)-; 1-(3,3-dimethylbutyl)-3-(2-fluoro-4-methyl-5-(7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)urea; Urea, N-(3,3-dimethylbutyl)-N'-[2-fluoro-4-methyl-5-[7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl]phenyl]-; GTPL8943; SCHEMBL15241297; CHEBI:167662; BCP23869; EX-A1638; BDBM50096279; DP4978; NSC781761; NSC801010; s7842; ZINC205861291; CCG-268937; NSC-781761; NSC-801010; SB16924; NCGC00481604-01; AC-30240; AS-74984; HY-12558; QC-11801; DP-4978;LY-3009120; J3.580.324F; C72761; Q27082823; B2693-470864; 1-(2-Fluoro-4-methyl-5-(2-methylamino-7-methylpyrido[2,3-d]pyrimidine-6-yl)phenyl)-3-(3,3-dimethylbutyl)urea; 3-(3,3-DIMETHYLBUTYL)-1-{2-FLUORO-4-METHYL-5-[7-METHYL-2-(METHYLAMINO)PYRIDO[2,3-D]PYRIMIDIN-6-YL]PHENYL}UREA; 4Z5
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Indication |
In total 1 Indication(s)
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Structure | |||||
Drug Resistance Disease(s) |
Disease(s) with Resistance Information Discovered by Cell Line Test for This Drug
(1 diseases)
Melanoma [ICD-11: 2C30]
[2]
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Target | Serine/threonine-protein kinase Raf (RAF) |
ARAF_HUMAN
; BRAF_HUMAN ; RAF1_HUMAN |
[1] | ||
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Formula |
6
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IsoSMILES |
CC1=CC(=C(C=C1C2=C(N=C3C(=C2)C=NC(=N3)NC)C)NC(=O)NCCC(C)(C)C)F
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InChI |
InChI=1S/C23H29FN6O/c1-13-9-18(24)19(29-22(31)26-8-7-23(3,4)5)11-16(13)17-10-15-12-27-21(25-6)30-20(15)28-14(17)2/h9-12H,7-8H2,1-6H3,(H2,26,29,31)(H,25,27,28,30)
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InChIKey |
HHCBMISMPSAZBF-UHFFFAOYSA-N
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PubChem CID |
Type(s) of Resistant Mechanism of This Drug
ADTT: Aberration of the Drug's Therapeutic Target
UAPP: Unusual Activation of Pro-survival Pathway
Drug Resistance Data Categorized by Their Corresponding Diseases
ICD-02: Benign/in-situ/malignant neoplasm
Solid tumour/cancer [ICD-11: 2A00-2F9Z]
Drug Sensitivity Data Categorized by Their Corresponding Mechanisms | ||||
Unusual Activation of Pro-survival Pathway (UAPP) | ||||
Key Molecule: Serine/threonine-protein kinase B-raf (BRAF) | [3] | |||
Molecule Alteration | IF-deletion | p.L485_P490delLNVTAP (c.1453_1470del18) |
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Sensitive Disease | Solid tumour/cancer [ICD-11: 2A00-2F9Z] | |||
Experimental Note | Revealed Based on the Cell Line Data | |||
In Vitro Model | HCT116 cells | Colon | Homo sapiens (Human) | CVCL_0291 |
A375 cells | Skin | Homo sapiens (Human) | CVCL_0132 | |
BxPC-3 cells | Pancreas | Homo sapiens (Human) | CVCL_0186 | |
NIH 3T3 cells | Colon | Homo sapiens (Human) | CVCL_0594 | |
HEK 293 cells | Kidney | Homo sapiens (Human) | CVCL_0045 | |
OV-90 cells | Ascites | Homo sapiens (Human) | CVCL_3768 | |
H2405 cells | Lung | Homo sapiens (Human) | CVCL_1551 | |
In Vivo Model | NIH nude rat xenograft model | Rattus norvegicus | ||
Experiment for Molecule Alteration |
Western blotting analysis | |||
Experiment for Drug Resistance |
CellTiter-Glo assay; Colony transformation assay; Cell-cycle analysis; BrdUrd incorporation assay |
Hematologic cancer [ICD-11: 2B3Z]
Drug Sensitivity Data Categorized by Their Corresponding Mechanisms | ||||
Aberration of the Drug's Therapeutic Target (ADTT) | ||||
Key Molecule: Serine/threonine-protein kinase B-raf (BRAF) | [3] | |||
Molecule Alteration | Missense mutation | p.K601N (c.1803A>C) |
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Sensitive Disease | Hematologic Cancer [ICD-11: MG24.Y] | |||
Experimental Note | Revealed Based on the Cell Line Data | |||
In Vitro Model | HCT116 cells | Colon | Homo sapiens (Human) | CVCL_0291 |
A375 cells | Skin | Homo sapiens (Human) | CVCL_0132 | |
BxPC-3 cells | Pancreas | Homo sapiens (Human) | CVCL_0186 | |
NIH 3T3 cells | Colon | Homo sapiens (Human) | CVCL_0594 | |
HEK 293 cells | Kidney | Homo sapiens (Human) | CVCL_0045 | |
OV-90 cells | Ascites | Homo sapiens (Human) | CVCL_3768 | |
H2405 cells | Lung | Homo sapiens (Human) | CVCL_1551 | |
In Vivo Model | NIH nude rat xenograft model | Rattus norvegicus | ||
Experiment for Molecule Alteration |
Western blotting analysis | |||
Experiment for Drug Resistance |
CellTiter-Glo assay; Colony transformation assay; Cell-cycle analysis; BrdUrd incorporation assay |
Pancreatic cancer [ICD-11: 2C10]
Drug Sensitivity Data Categorized by Their Corresponding Mechanisms | ||||
Aberration of the Drug's Therapeutic Target (ADTT) | ||||
Key Molecule: Serine/threonine-protein kinase B-raf (BRAF) | [3] | |||
Molecule Alteration | Complex-indel | p.V487_P492delinsA (c.1460_1474del15) |
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Sensitive Disease | Pancreatic ductal adenocarcinoma [ICD-11: 2C10.0] | |||
Experimental Note | Revealed Based on the Cell Line Data | |||
In Vitro Model | HCT116 cells | Colon | Homo sapiens (Human) | CVCL_0291 |
A375 cells | Skin | Homo sapiens (Human) | CVCL_0132 | |
BxPC-3 cells | Pancreas | Homo sapiens (Human) | CVCL_0186 | |
NIH 3T3 cells | Colon | Homo sapiens (Human) | CVCL_0594 | |
HEK 293 cells | Kidney | Homo sapiens (Human) | CVCL_0045 | |
OV-90 cells | Ascites | Homo sapiens (Human) | CVCL_3768 | |
H2405 cells | Lung | Homo sapiens (Human) | CVCL_1551 | |
In Vivo Model | NIH nude rat xenograft model | Rattus norvegicus | ||
Experiment for Molecule Alteration |
Western blotting analysis | |||
Experiment for Drug Resistance |
CellTiter-Glo assay; Colony transformation assay; Cell-cycle analysis; BrdUrd incorporation assay |
Lung cancer [ICD-11: 2C25]
Drug Sensitivity Data Categorized by Their Corresponding Mechanisms | ||||
Aberration of the Drug's Therapeutic Target (ADTT) | ||||
Key Molecule: Serine/threonine-protein kinase B-raf (BRAF) | [3] | |||
Molecule Alteration | Complex-indel | p.L485_P490delinsY (c.1453_1470delinsTAT) |
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Sensitive Disease | Lung adenocarcinoma [ICD-11: 2C25.0] | |||
Experimental Note | Revealed Based on the Cell Line Data | |||
In Vitro Model | HCT116 cells | Colon | Homo sapiens (Human) | CVCL_0291 |
A375 cells | Skin | Homo sapiens (Human) | CVCL_0132 | |
BxPC-3 cells | Pancreas | Homo sapiens (Human) | CVCL_0186 | |
NIH 3T3 cells | Colon | Homo sapiens (Human) | CVCL_0594 | |
HEK 293 cells | Kidney | Homo sapiens (Human) | CVCL_0045 | |
OV-90 cells | Ascites | Homo sapiens (Human) | CVCL_3768 | |
H2405 cells | Lung | Homo sapiens (Human) | CVCL_1551 | |
In Vivo Model | NIH nude rat xenograft model | Rattus norvegicus | ||
Experiment for Molecule Alteration |
Western blotting analysis | |||
Experiment for Drug Resistance |
CellTiter-Glo assay; Colony transformation assay; Cell-cycle analysis; BrdUrd incorporation assay |
Melanoma [ICD-11: 2C30]
Drug Resistance Data Categorized by Their Corresponding Mechanisms | ||||
Unusual Activation of Pro-survival Pathway (UAPP) | ||||
Key Molecule: GTPase Nras (NRAS) | [2] | |||
Molecule Alteration | Missense mutation | p.Q61L (c.182A>T) |
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Resistant 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 |
Sk-Mel28 cells | Skin | Homo sapiens (Human) | CVCL_0526 | |
A2058 cells | Skin | Homo sapiens (Human) | CVCL_1059 | |
A375 cells | Skin | Homo sapiens (Human) | CVCL_0132 | |
A375 cells | Skin | Homo sapiens (Human) | CVCL_0132 | |
A375 cells | Skin | Homo sapiens (Human) | CVCL_0132 | |
WM2664 cells | Skin | Homo sapiens (Human) | CVCL_2765 | |
SkMEL 30 cells | Skin | Homo sapiens (Human) | CVCL_0039 | |
SkMEL 2 cells | Skin | Homo sapiens (Human) | CVCL_0069 | |
SH4 cells | Skin | Mus musculus (Mouse) | CVCL_7702 | |
MEXF-535 cells | Skin | Homo sapiens (Human) | N.A. | |
MEXF-1792 cells | Skin | Homo sapiens (Human) | N.A. | |
MEXF-1341 cells | Skin | Homo sapiens (Human) | N.A. | |
M14 cells | Hypodermis | Homo sapiens (Human) | CVCL_1395 | |
GAK cells | Lnguinal lymph node | Homo sapiens (Human) | CVCL_1225 | |
Colo829 cells | Skin | Homo sapiens (Human) | CVCL_1137 | |
In Vivo Model | Female NIH nude mouse xenograft model | Mus musculus | ||
Experiment for Molecule Alteration |
Western blotting analysis; Crystallization assay; X-ray data collection and structure determination assay | |||
Experiment for Drug Resistance |
CellTiter-Glo assay; Enzymatic kinase assay |
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.L597S (c.1789_1790delCTinsTC) |
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Sensitive Disease | Melanoma [ICD-11: 2C30.0] | |||
Experimental Note | Identified from the Human Clinical Data | |||
Cell Pathway Regulation | MAPK signaling pathway | Inhibition | hsa04010 | |
In Vitro Model | Skin sample | N.A. | ||
In Vivo Model | Mouse PDX model | Mus musculus | ||
Experiment for Drug Resistance |
Crystal violet staining assay | |||
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 |
Sk-Mel28 cells | Skin | Homo sapiens (Human) | CVCL_0526 | |
A2058 cells | Skin | Homo sapiens (Human) | CVCL_1059 | |
A375 cells | Skin | Homo sapiens (Human) | CVCL_0132 | |
A375 cells | Skin | Homo sapiens (Human) | CVCL_0132 | |
A375 cells | Skin | Homo sapiens (Human) | CVCL_0132 | |
WM2664 cells | Skin | Homo sapiens (Human) | CVCL_2765 | |
SkMEL 30 cells | Skin | Homo sapiens (Human) | CVCL_0039 | |
SkMEL 2 cells | Skin | Homo sapiens (Human) | CVCL_0069 | |
SH4 cells | Skin | Mus musculus (Mouse) | CVCL_7702 | |
MEXF-535 cells | Skin | Homo sapiens (Human) | N.A. | |
MEXF-1792 cells | Skin | Homo sapiens (Human) | N.A. | |
MEXF-1341 cells | Skin | Homo sapiens (Human) | N.A. | |
M14 cells | Hypodermis | Homo sapiens (Human) | CVCL_1395 | |
GAK cells | Lnguinal lymph node | Homo sapiens (Human) | CVCL_1225 | |
Colo829 cells | Skin | Homo sapiens (Human) | CVCL_1137 | |
In Vivo Model | Female NIH nude mouse xenograft model | Mus musculus | ||
Experiment for Molecule Alteration |
Western blotting analysis; Crystallization assay; X-ray data collection and structure determination assay | |||
Experiment for Drug Resistance |
CellTiter-Glo assay; Enzymatic kinase assay | |||
Key Molecule: GTPase Nras (NRAS) | [2] | |||
Molecule Alteration | Missense mutation | p.Q61K (c.181C>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 |
Sk-Mel28 cells | Skin | Homo sapiens (Human) | CVCL_0526 | |
A2058 cells | Skin | Homo sapiens (Human) | CVCL_1059 | |
A375 cells | Skin | Homo sapiens (Human) | CVCL_0132 | |
A375 cells | Skin | Homo sapiens (Human) | CVCL_0132 | |
A375 cells | Skin | Homo sapiens (Human) | CVCL_0132 | |
WM2664 cells | Skin | Homo sapiens (Human) | CVCL_2765 | |
SkMEL 30 cells | Skin | Homo sapiens (Human) | CVCL_0039 | |
SkMEL 2 cells | Skin | Homo sapiens (Human) | CVCL_0069 | |
SH4 cells | Skin | Mus musculus (Mouse) | CVCL_7702 | |
MEXF-535 cells | Skin | Homo sapiens (Human) | N.A. | |
MEXF-1792 cells | Skin | Homo sapiens (Human) | N.A. | |
MEXF-1341 cells | Skin | Homo sapiens (Human) | N.A. | |
M14 cells | Hypodermis | Homo sapiens (Human) | CVCL_1395 | |
GAK cells | Lnguinal lymph node | Homo sapiens (Human) | CVCL_1225 | |
Colo829 cells | Skin | Homo sapiens (Human) | CVCL_1137 | |
In Vivo Model | Female NIH nude mouse xenograft model | Mus musculus | ||
Experiment for Molecule Alteration |
Western blotting analysis; Crystallization assay; X-ray data collection and structure determination assay | |||
Experiment for Drug Resistance |
CellTiter-Glo assay; Enzymatic kinase assay | |||
Key Molecule: GTPase Nras (NRAS) | [2] | |||
Molecule Alteration | Missense mutation | p.G13D (c.38G>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 |
Sk-Mel28 cells | Skin | Homo sapiens (Human) | CVCL_0526 | |
A2058 cells | Skin | Homo sapiens (Human) | CVCL_1059 | |
A375 cells | Skin | Homo sapiens (Human) | CVCL_0132 | |
A375 cells | Skin | Homo sapiens (Human) | CVCL_0132 | |
A375 cells | Skin | Homo sapiens (Human) | CVCL_0132 | |
WM2664 cells | Skin | Homo sapiens (Human) | CVCL_2765 | |
SkMEL 30 cells | Skin | Homo sapiens (Human) | CVCL_0039 | |
SkMEL 2 cells | Skin | Homo sapiens (Human) | CVCL_0069 | |
SH4 cells | Skin | Mus musculus (Mouse) | CVCL_7702 | |
MEXF-535 cells | Skin | Homo sapiens (Human) | N.A. | |
MEXF-1792 cells | Skin | Homo sapiens (Human) | N.A. | |
MEXF-1341 cells | Skin | Homo sapiens (Human) | N.A. | |
M14 cells | Hypodermis | Homo sapiens (Human) | CVCL_1395 | |
GAK cells | Lnguinal lymph node | Homo sapiens (Human) | CVCL_1225 | |
Colo829 cells | Skin | Homo sapiens (Human) | CVCL_1137 | |
In Vivo Model | Female NIH nude mouse xenograft model | Mus musculus | ||
Experiment for Molecule Alteration |
Western blotting analysis; Crystallization assay; X-ray data collection and structure determination assay | |||
Experiment for Drug Resistance |
CellTiter-Glo assay; Enzymatic kinase assay | |||
Key Molecule: Cellular tumor antigen p53 (TP53) | [2] | |||
Molecule Alteration | Missense mutation | p.D259Y (c.775G>T) |
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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 |
Sk-Mel28 cells | Skin | Homo sapiens (Human) | CVCL_0526 | |
A2058 cells | Skin | Homo sapiens (Human) | CVCL_1059 | |
A375 cells | Skin | Homo sapiens (Human) | CVCL_0132 | |
A375 cells | Skin | Homo sapiens (Human) | CVCL_0132 | |
A375 cells | Skin | Homo sapiens (Human) | CVCL_0132 | |
WM2664 cells | Skin | Homo sapiens (Human) | CVCL_2765 | |
SkMEL 30 cells | Skin | Homo sapiens (Human) | CVCL_0039 | |
SkMEL 2 cells | Skin | Homo sapiens (Human) | CVCL_0069 | |
SH4 cells | Skin | Mus musculus (Mouse) | CVCL_7702 | |
MEXF-535 cells | Skin | Homo sapiens (Human) | N.A. | |
MEXF-1792 cells | Skin | Homo sapiens (Human) | N.A. | |
MEXF-1341 cells | Skin | Homo sapiens (Human) | N.A. | |
M14 cells | Hypodermis | Homo sapiens (Human) | CVCL_1395 | |
GAK cells | Lnguinal lymph node | Homo sapiens (Human) | CVCL_1225 | |
Colo829 cells | Skin | Homo sapiens (Human) | CVCL_1137 | |
In Vivo Model | Female NIH nude mouse xenograft model | Mus musculus | ||
Experiment for Molecule Alteration |
Western blotting analysis; Crystallization assay; X-ray data collection and structure determination assay | |||
Experiment for Drug Resistance |
CellTiter-Glo assay; Enzymatic kinase assay |
Ovarian cancer [ICD-11: 2C73]
Drug Sensitivity Data Categorized by Their Corresponding Mechanisms | ||||
Unusual Activation of Pro-survival Pathway (UAPP) | ||||
Key Molecule: Serine/threonine-protein kinase B-raf (BRAF) | [3] | |||
Molecule Alteration | IF-deletion | p.N486_P490delNVTAP (c.1457_1471del15) |
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Sensitive Disease | Ovarian cancer [ICD-11: 2C73.0] | |||
Experimental Note | Revealed Based on the Cell Line Data | |||
In Vitro Model | HCT116 cells | Colon | Homo sapiens (Human) | CVCL_0291 |
A375 cells | Skin | Homo sapiens (Human) | CVCL_0132 | |
BxPC-3 cells | Pancreas | Homo sapiens (Human) | CVCL_0186 | |
NIH 3T3 cells | Colon | Homo sapiens (Human) | CVCL_0594 | |
HEK 293 cells | Kidney | Homo sapiens (Human) | CVCL_0045 | |
OV-90 cells | Ascites | Homo sapiens (Human) | CVCL_3768 | |
H2405 cells | Lung | Homo sapiens (Human) | CVCL_1551 | |
In Vivo Model | NIH nude rat xenograft model | Rattus norvegicus | ||
Experiment for Molecule Alteration |
Western blotting analysis | |||
Experiment for Drug Resistance |
CellTiter-Glo assay; Colony transformation assay; Cell-cycle analysis; BrdUrd incorporation assay |
References
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