Therapy Detail

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Therapy Name CI-1040
Synonyms
Therapy Description

CI-1040 (PD184352) binds and inhibits Mek1 and Mek2, which may inhibit the activation of downstream signaling targets and reduce tumor cell proliferation (PMID: 14613031, PMID: 16009947).

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Drug Name Trade Name Synonyms Drug Classes Drug Description
CI-1040 PD184352|PD-184352 MEK inhibitor (Pan) 23 MEK1 Inhibitor 25 MEK2 Inhibitor 23 CI-1040 (PD184352) binds and inhibits Mek1 and Mek2, which may inhibit the activation of downstream signaling targets and reduce tumor cell proliferation (PMID: 14613031, PMID: 16009947).

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Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
BRAF V600E ovarian cancer sensitive CI-1040 Preclinical - Cell line xenograft Actionable In a preclinical study, CI-1040 inhibited growth of a human ovarian cancer cell line harboring BRAF V600E in culture, and inhibited tumor growth in xenograft models (PMID: 19018267). 19018267
HRAS G12V melanoma sensitive CI-1040 Preclinical Actionable In a preclinical study CI-1040 (PD-184352) inhibited melanoma progression in a transgenic zebrafish model of melanoma expressing HRAS G12V (PMID: 26267534). 26267534
MAP2K1 L118Q Advanced Solid Tumor predicted - resistant CI-1040 Preclinical - Biochemical Actionable In a preclinical study, CI-1040 (PD184352) did not inhibit kinase activity of MAP2K1 L118Q in an in vitro assay (PMID: 12370306). 12370306
MAP2K1 I111R Advanced Solid Tumor predicted - resistant CI-1040 Preclinical - Biochemical Actionable In a preclinical study, CI-1040 (PD184352) did not inhibit kinase activity of MAP2K1 I111R in an in vitro assay (PMID: 12370306). 12370306
BRAF V600E MAP2K1 I99T melanoma resistant CI-1040 Preclinical - Cell culture Actionable In a preclinical study, expression of MAP2K1 I99T in melanoma cells harboring BRAF V600E conferred resistance to CI-1040 (PD184352) treatment in culture (PMID: 19915144). 19915144
MAP2K1 I139R Advanced Solid Tumor decreased response CI-1040 Preclinical - Biochemical Actionable In a preclinical study, MAP2K1 I139R demonstrated decreased sensitivity to CI-1040 (PD184352) in an in vitro kinase assay (PMID: 12370306). 12370306
MAP2K1 I103N Advanced Solid Tumor decreased response CI-1040 Preclinical - Biochemical Actionable In a preclinical study, MAP2K1 I103N demonstrated decreased sensitivity to CI-1040 (PD184352) in an in vitro kinase assay (PMID: 12370306). 12370306
BRAF T529I BRAF V600E Advanced Solid Tumor sensitive CI-1040 Preclinical Actionable In a preclinical study, CI-1040 (PD184352) inhibited Erk phosphorylation in transformed cells expressing BRAF V600E and the gatekeeper mutation BRAF T529I in culture (PMID: 20538618). 20538618
MAP2K1 L118P Advanced Solid Tumor predicted - resistant CI-1040 Preclinical - Biochemical Actionable In a preclinical study, CI-1040 (PD184352) did not inhibit kinase activity of MAP2K1 L118P in an in vitro assay (PMID: 12370306). 12370306
BRAF T529M BRAF V600E Advanced Solid Tumor predicted - sensitive CI-1040 Preclinical Actionable In a preclinical study, CI-1040 (PD184352) inhibited Erk phosphorylation in transformed cells expressing BRAF V600E and the gatekeeper mutation BRAF T529M in culture (PMID: 20538618). 20538618
MAP2K1 L115P Advanced Solid Tumor resistant CI-1040 Preclinical - Biochemical Actionable In a preclinical study, CI-1040 (PD184352) did not inhibit kinase activity of MAP2K1 L115P in an in vitro assay and failed to suppress Erk phosphorylation in cells expressing MAP2K1 L115P in culture (PMID: 12370306). 12370306
BRAF V600E MAP2K1 I103N melanoma resistant CI-1040 Preclinical - Cell culture Actionable In a preclinical study, expression of MAP2K1 I103N in melanoma cells harboring BRAF V600E conferred resistance to CI-1040 (PD184352) treatment in culture (PMID: 19915144). 19915144
MAP2K1 I139G Advanced Solid Tumor predicted - resistant CI-1040 Preclinical - Biochemical Actionable In a preclinical study, CI-1040 (PD184352) did not inhibit kinase activity of MAP2K1 I139G in an in vitro assay (PMID: 12370306). 12370306
BRAF T529N BRAF V600E Advanced Solid Tumor sensitive CI-1040 Preclinical Actionable In a preclinical study, CI-1040 (PD184352) inhibited Erk phosphorylation and growth of transformed cells expressing BRAF V600E and the gatekeeper mutation BRAF T529N in culture (PMID: 20538618). 20538618
BRAF V600E MAP2K1 V211D melanoma resistant CI-1040 Preclinical Actionable In a preclinical study, expression of MAP2K1 V211D in melanoma cells harboring BRAF V600E conferred resistance to CI-1040 (PD184352) treatment in culture (PMID: 19915144). 19915144
MAP2K1 L115A Advanced Solid Tumor decreased response CI-1040 Preclinical - Biochemical Actionable In a preclinical study, MAP2K1 L115A demonstrated decreased sensitivity to CI-1040 (PD184352) in an in vitro kinase assay (PMID: 12370306). 12370306
MAP2K1 I139N Advanced Solid Tumor decreased response CI-1040 Preclinical - Biochemical Actionable In a preclinical study, MAP2K1 I139N demonstrated decreased sensitivity to CI-1040 (PD184352) in an in vitro kinase assay (PMID: 12370306). 12370306
MAP2K1 F53S Advanced Solid Tumor sensitive CI-1040 Preclinical - Biochemical Actionable In a preclinical study, CI-1040 (PD184352) inhibited kinase activity of MAP2K1 F53S in an in vitro assay and decreased Erk phosphorylation in cells expressing MAP2K1 F53S in culture (PMID: 12370306). 12370306
BRAF V600E MAP2K1 I111N melanoma resistant CI-1040 Preclinical - Cell culture Actionable In a preclinical study, expression of MAP2K1 I111N in melanoma cells harboring BRAF V600E conferred resistance to CI-1040 (PD184352) treatment in culture (PMID: 19915144). 19915144
BRAF V600E MAP2K1 L115P melanoma resistant CI-1040 Preclinical - Cell culture Actionable In a preclinical study, expression of MAP2K1 L115P in melanoma cells harboring BRAF V600E conferred resistance to CI-1040 (PD184352) treatment in culture (PMID: 19915144). 19915144
BRAF V600E MAP2K1 H119P melanoma resistant CI-1040 Preclinical - Cell culture Actionable In a preclinical study, expression of MAP2K1 H119P in melanoma cells harboring BRAF V600E conferred resistance to CI-1040 (PD184352) treatment in culture (PMID: 19915144). 19915144
MAP2K1 I111A Advanced Solid Tumor decreased response CI-1040 Preclinical - Biochemical Actionable In a preclinical study, MAP2K1 I111A demonstrated decreased sensitivity to CI-1040 (PD184352) in an in vitro kinase assay (PMID: 12370306). 12370306
BRAF V600E Advanced Solid Tumor sensitive CI-1040 Preclinical Actionable In a preclinical study, CI-1040 (PD184352) inhibited Erk phosphorylation and growth of transformed cells expressing BRAF V600E in culture (PMID: 20538618). 20538618
MAP2K1 I111D Advanced Solid Tumor predicted - resistant CI-1040 Preclinical - Biochemical Actionable In a preclinical study, CI-1040 (PD184352) did not inhibit kinase activity of MAP2K1 I111D in an in vitro assay (PMID: 12370306). 12370306
BRAF V600E MAP2K1 L115R melanoma resistant CI-1040 Preclinical - Cell culture Actionable In a preclinical study, expression of MAP2K1 L115R in melanoma cells harboring BRAF V600E conferred resistance to CI-1040 (PD184352) treatment in culture (PMID: 19915144). 19915144
MAP2K1 I111P Advanced Solid Tumor predicted - resistant CI-1040 Preclinical - Biochemical Actionable In a preclinical study, CI-1040 (PD184352) did not inhibit kinase activity of MAP2K1 I111P in an in vitro assay (PMID: 12370306). 12370306
MAP2K1 L118D Advanced Solid Tumor predicted - resistant CI-1040 Preclinical - Biochemical Actionable In a preclinical study, CI-1040 (PD184352) did not inhibit kinase activity of MAP2K1 L118D in an in vitro assay (PMID: 12370306). 12370306
MAP2K1 L118G Advanced Solid Tumor decreased response CI-1040 Preclinical - Biochemical Actionable In a preclinical study, MAP2K1 L118G demonstrated decreased sensitivity to CI-1040 (PD184352) in an in vitro kinase assay (PMID: 12370306). 12370306

Filtering

  • Case insensitive filtering will display rows if any text in any cell matches the filter term
  • Use simple literal full or partial string matches
  • Separate multiple filter terms with a space. Any order may be used (i. e. a b c and c b a are equivalent )
  • Filtering will only apply to rows that are already loaded on the page. Filtering has no impact on query parameters.
  • Use quotes to match on a longer phrase with spaces (i.e. "mtor c1483f")

Sorting

  • Generally, the default sort order for tables is set to be first column ascending; however, specific tables may set a different default sort order.
  • Click on any column header arrows to sort by that column
  • Hold down the Shift key and click multiple columns to sort by more than one column. Be sure to set ascending or descending order for a given column before moving on to the next column.

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