Drug Information

Drug (ID: DG01699) and It's Reported Resistant Information
Name
MK2206/Temsirolimus
Synonyms
MK2206/Temsirolimus
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Target . NOUNIPROTAC [1]
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
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Thyroid cancer [ICD-11: 2D10]
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Drug Sensitivity Data Categorized by Their Corresponding Mechanisms
       Unusual Activation of Pro-survival Pathway (UAPP) Click to Show/Hide
Key Molecule: PI3-kinase alpha (PIK3CA) [1]
Molecule Alteration Missense mutation
p.H1047R (c.3140A>G)
 Molecule Info 
Sensitive Disease Thyroid gland cancer [ICD-11: 2D10.0]
 Disease Info 
Experimental Note Revealed Based on the Cell Line Data
In Vitro Model SW1736 cells Thyroid Homo sapiens (Human) CVCL_3883
C643 cells Thyroid gland Homo sapiens (Human) CVCL_5969
HTH7 cells Thyroid gland Homo sapiens (Human) CVCL_6289
Hth74 cells Thyroid gland Homo sapiens (Human) CVCL_6288
Experiment for
Molecule Alteration		 Western blotting analysis
Experiment for
Drug Resistance		 MTT assay
Mechanism Description The missense mutation p.H1047R (c.3140A>G) in gene PIK3CA cause the sensitivity of MK2206 + Temsirolimus by unusual activation of pro-survival pathway
Key Molecule: PI3-kinase alpha (PIK3CA) [1]
Molecule Alteration Missense mutation
p.E542K (c.1624G>A)
 Molecule Info 
Sensitive Disease Thyroid gland cancer [ICD-11: 2D10.0]
 Disease Info 
Experimental Note Revealed Based on the Cell Line Data
In Vitro Model SW1736 cells Thyroid Homo sapiens (Human) CVCL_3883
C643 cells Thyroid gland Homo sapiens (Human) CVCL_5969
HTH7 cells Thyroid gland Homo sapiens (Human) CVCL_6289
Hth74 cells Thyroid gland Homo sapiens (Human) CVCL_6288
Experiment for
Molecule Alteration		 Western blotting analysis
Experiment for
Drug Resistance		 MTT assay
Mechanism Description The missense mutation p.E542K (c.1624G>A) in gene PIK3CA cause the sensitivity of MK2206 + Temsirolimus by unusual activation of pro-survival pathway
References
Ref 1 The Akt-specific inhibitor MK2206 selectively inhibits thyroid cancer cells harboring mutations that can activate the PI3K/Akt pathwayJ Clin Endocrinol Metab. 2011 Apr;96(4):E577-85. doi: 10.1210/jc.2010-2644. Epub 2011 Feb 2.

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