Drug Information

Drug (ID: DG01474) and It's Reported Resistant Information
Name
Perifosine
Synonyms
Perifosine; 157716-52-4; KRX-0401; 1,1-Dimethylpiperidin-1-ium-4-yl octadecyl phosphate; (1,1-dimethylpiperidin-1-ium-4-yl) octadecyl phosphate; Perifosine (KRX-0401); NSC 639966; D 21266; 1,1-dimethylpiperidinium-4-yl octadecyl phosphate; UNII-2GWV496552; KRX 0401; NSC639966; D-21266; NSC-639966; CHEBI:67272; 2GWV496552; NCGC00187909-01; Piperidinium, 4-[[hydroxy(octadecyloxy)phosphinyl]oxy]-1,1-dimethyl-, inner salt; 1,1-dimethylpiperidin-1-ium-4-yl octadecyl phosphate.; Piperidinium, 4-((hydroxy(octadecyloxy)phosphinyl)oxy)-1,1-dimethyl-, inner salt; Perifosine [INN]; NKA17; C25H52NO4P; octadecyl-(1,1-dimethyl-4-piperidylio)phosphate; 4-((Hydroxy(octadecyloxy)phosphinyl)oxy)-1,1-dimethylpiperidinium inner salt; DSSTox_CID_28872; DSSTox_RID_83141; DSSTox_GSID_48946; SCHEMBL93872; CHEMBL372764; GTPL7424; DTXSID3048946; AOB3006; QCR-270; BCP00245; EX-A2229; YHI-1003; Tox21_113365; BDBM50431630; MFCD00927554; NSC800842; s1037; Piperidinium,1-dimethyl-, inner salt; AKOS005146344; CCG-269358; CS-0209; DB06641; EX-3388; GS-3834; NSC-800842; NCGC00187909-02; NCGC00187909-13; AC-25019; AM808092; HY-50909; CAS-157716-52-4; FT-0651459; W3423; A23834; D21266; Octadecyl-(1,1-dimethyl-4-piperidylio) phosphate; J-500086; Q3411917; Perifosine; KRX-0401; NSC 639966; D21266; 4-Hydroxy-1,1-dimethylpiperidinium hydroxide, octadecyl hydrogen phosphate, inner salt
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Indication
In total 3 Indication(s)
Solid tumour/cancer [ICD-11: 2A00-2F9Z]
Phase 1
[1]
Solid tumour/cancer [ICD-11: 2A00-2F9Z]
Phase 1
[1]
Solid tumour/cancer [ICD-11: 2A00-2F9Z]
Phase 1
[1]
Structure
Target Tubulin (TUB) NOUNIPROTAC [1]
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Formula
20
IsoSMILES
CCCCCCCCCCCCCCCCCCOP(=O)([O-])OC1CC[N+](CC1)(C)C
InChI
InChI=1S/C25H52NO4P/c1-4-5-6-7-8-9-10-11-12-13-14-15-16-17-18-19-24-29-31(27,28)30-25-20-22-26(2,3)23-21-25/h25H,4-24H2,1-3H3
InChIKey
SZFPYBIJACMNJV-UHFFFAOYSA-N
PubChem CID
148177
ChEBI ID
CHEBI:67272
TTD Drug ID
D0O5WP
DrugBank ID
DB06641
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: Phosphatase and tensin homolog (PTEN) [1]
Molecule Alteration Nonsense
p.R130* (c.388C>T)
 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
SW1736 cells Thyroid Homo sapiens (Human) CVCL_3883
HTH7 cells Thyroid gland Homo sapiens (Human) CVCL_6289
Hth74 cells Thyroid gland Homo sapiens (Human) CVCL_6288
Hth74 cells Thyroid gland Homo sapiens (Human) CVCL_6288
In Vivo Model Nude mouse xenograft model Mus musculus
Experiment for
Molecule Alteration		 Western blotting analysis
Experiment for
Drug Resistance		 MTT assay
Mechanism Description The nonsense p.R130* (c.388C>T) in gene PTEN cause the sensitivity of Perifosine 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
SW1736 cells Thyroid Homo sapiens (Human) CVCL_3883
HTH7 cells Thyroid gland Homo sapiens (Human) CVCL_6289
Hth74 cells Thyroid gland Homo sapiens (Human) CVCL_6288
Hth74 cells Thyroid gland Homo sapiens (Human) CVCL_6288
In Vivo Model Nude mouse xenograft model Mus musculus
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 Perifosine by unusual activation of pro-survival pathway
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
SW1736 cells Thyroid Homo sapiens (Human) CVCL_3883
HTH7 cells Thyroid gland Homo sapiens (Human) CVCL_6289
Hth74 cells Thyroid gland Homo sapiens (Human) CVCL_6288
Hth74 cells Thyroid gland Homo sapiens (Human) CVCL_6288
In Vivo Model Nude mouse xenograft model Mus musculus
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 Perifosine by unusual activation of pro-survival pathway
References
Ref 1 Genetic alterations in the phosphoinositide 3-kinase/Akt signaling pathway confer sensitivity of thyroid cancer cells to therapeutic targeting of Akt and mammalian target of rapamycinCancer Res. 2009 Sep 15;69(18):7311-9. doi: 10.1158/0008-5472.CAN-09-1077. Epub 2009 Aug 25.

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