Therapy Detail

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Therapy Name SHP099
Synonyms
Therapy Description

SHP099 is an allosteric inhibitor of SHP2 that stabilizes SHP2 in its autoinhibited conformation, which reduces downstream signaling and potentially leads to decreased growth of receptor tyrosine kinase-driven tumors (PMID: 27362227).

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Drug Name Trade Name Synonyms Drug Classes Drug Description
SHP099 SHP2 Inhibitor 9 SHP099 is an allosteric inhibitor of SHP2 that stabilizes SHP2 in its autoinhibited conformation, which reduces downstream signaling and potentially leads to decreased growth of receptor tyrosine kinase-driven tumors (PMID: 27362227, PMID: 31043123).

Filtering

  • Case insensitive filtering will display rows where any text in any cell matches the filter term
  • Simple literal full or partial string matches
  • Separate multiple filter terms with a spaces, order doesn't matter (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 a longer phrase which contains spaces "mtor c1483f"

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Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
BRAF V600E colorectal cancer resistant SHP099 Preclinical - Cell culture Actionable In a preclincial study, colorectal cancer cell lines harboring BRAF V600E demonstrated resistance to SHP099 in culture (PMID: 27362227). 27362227
NRAS mutant hematologic cancer predicted - resistant SHP099 Preclinical Actionable In a preclinical study, hematopoietic cancer cell lines harboring NRAS mutations demonstrated resistance to SHP099 in cell culture (PMID: 27362227). 27362227
FLT3 exon 14 ins acute myeloid leukemia predicted - sensitive SHP099 Preclinical - Pdx Actionable In a preclinical study, treatment with SHP099 resulted in reduction of CD45-positive leukemic cells and decreased splenomegaly in a human primary tumor-derived xenograft model of acute myeloid leukemia harboring a FLT3-ITD mutation (PMID: 27362227). 27362227
PTPN11 E76K myeloid leukemia resistant SHP099 Preclinical - Cell culture Actionable In a preclinical study, SHP099 had no effect on Erk1/2 phosphorylation, Bcl-xl expression, Parp cleavage, and growth of myeloid cells expressing PTPN11 E76K in culture (PMID: 29568093). 29568093
JAK2 V617F hematologic cancer sensitive SHP099 Preclinical - Cell culture Actionable In a preclinical study, SHP099 inhibited proliferation of a hematopoietic cancer cell line harboring JAK2 V617F in culture (PMID: 27362227). 27362227
PTPN11 E69K myeloid leukemia sensitive SHP099 Preclinical - Cell culture Actionable In a preclinical study, SHP099 inhibited Erk1/2 phosphorylation, Bcl-xl expression, Parp cleavage, and growth of myeloid cells expressing PTPN11 A72V in culture (PMID: 29568093). 29568093
PTPN11 dec exp myeloid leukemia resistant SHP099 Preclinical - Cell culture Actionable In a preclinical study, SHP099 had no effect on Erk1/2 phosphorylation, Bcl-xl expression, Parp cleavage, and growth of PTPN11 knock-out myeloid cells in culture (PMID: 29568093). 29568093
PTPN11 D61Y myeloid leukemia resistant SHP099 Preclinical - Cell culture Actionable In a preclinical study, SHP099 had no effect on Erk1/2 phosphorylation, Bcl-xl expression, Parp cleavage, and growth of myeloid cells expressing PTPN11 D61Y in culture (PMID: 29568093). 29568093
BRAF V600E melanoma no benefit SHP099 Preclinical Actionable In a preclinical study, SHP099 did not inhibit proliferation or ERK activation in a melanoma cell line harboring BRAF V600E in culture (PMID: 27362227). 27362227
PTPN11 A72V myeloid leukemia resistant SHP099 Preclinical - Cell culture Actionable In a preclinical study, SHP099 had no effect on Erk1/2 phosphorylation, Bcl-xl expression, Parp cleavage, and growth of myeloid cells expressing PTPN11 A72V in culture (PMID: 29568093). 29568093

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Clinical Trial Phase Therapies Title Recruitment Status


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