Therapy Detail

Request Content

Contact

Missing content? – Request curation!

Request curation for specific Genes, Variants, or PubMed publications.

Have questions, comments, or suggestions? - Let us know!

Email us at : ckbsupport@genomenon.com

Therapy Name	RAF265
Synonyms
Therapy Description	RAF265 inhibits the activities of several intracellular kinases, including BRAF(V600E), BRAF(wild type), c-RAF (RAF1), VEGF receptor 2 (VEGFR2/KDR), platelet-derived growth factor receptor (PDGFR), colony-stimulating factor (CSF)1R, RET and c-KIT, SRC, STE20, which may result in a reduction of tumor cell growth and proliferation, and tumor cell death (PMID: 22351689, PMID: 28719152).

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.

Filter rows:

Showing 1 to 1 of 1 entries

Drug Name	Trade Name	Synonyms	Drug Classes	Drug Description
RAF265		CHIR-265\|NVP-RAF265	BRAF Inhibitor 26 CRAF Inhibitor 12 VEGFR2 Inhibitor 37	RAF265 inhibits the activities of several intracellular kinases, including BRAF(V600E), BRAF(wild type), c-RAF (RAF1), VEGF receptor 2 (VEGFR2/KDR), platelet-derived growth factor receptor (PDGFR), colony-stimulating factor (CSF)1R, RET and c-KIT, SRC, STE20, which may result in a reduction of tumor cell growth and proliferation, and tumor cell death (PMID: 22351689, PMID: 28719152).

Showing 1 to 1 of 1 entries

Filter rows:

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.

Filter rows:

Showing 1 to 10 of 10 entries

Molecular Profile	Indication/Tumor Type	Response Type	Therapy Name	Approval Status	Evidence Type	Efficacy Evidence	References
BRAF wild-type	melanoma	predicted - sensitive	RAF265	Phase I	Actionable	In a Phase I trial, treatment with RAF265 in melanoma patients resulted in an objective response rate of 12.1% (8/66), including a partial response in four patients harboring BRAF V600E, two partial responses and one complete response in patients with wild-type BRAF, and one complete response in a patient with unknown mutational status (PMID: 28719152).	28719152
BRAF V600E	melanoma	predicted - sensitive	RAF265	Case Reports/Case Series	Actionable	In a Phase I trial, treatment with RAF265 in melanoma patients resulted in an objective response rate of 12.1% (8/66), including a partial response in four patients harboring BRAF V600E, two partial responses and one complete response in patients with wild-type BRAF, and one complete response in a patient with unknown mutational status (PMID: 28719152).	28719152
HRAS G12V	urinary bladder cancer	sensitive	RAF265	Preclinical - Cell culture	Actionable	In a preclinical study, RAF265 treatment decreased viability and colony formation of a bladder cancer cell line harboring HRAS G12V in culture (PMID: 34554931).	34554931
NRAS Q61L	urinary bladder cancer	sensitive	RAF265	Preclinical - Cell culture	Actionable	In a preclinical study, RAF265 treatment decreased colony formation of a bladder cancer cell line harboring NRAS Q61L in culture (PMID: 34554931).	34554931
NRAS Q61R	urinary bladder cancer	sensitive	RAF265	Preclinical - Cell culture	Actionable	In a preclinical study, RAF265 treatment decreased viability of a bladder cancer cell line harboring NRAS Q61R in culture (PMID: 34554931).	34554931
BRAF T529I BRAF V600E	Advanced Solid Tumor	predicted - sensitive	RAF265	Preclinical	Actionable	In a preclinical study, RAF265 inhibited kinase activity in vitro, and downstream Erk phosphorylation in cells expressing BRAF V600E and the gatekeeper mutation BRAF T529I to a similar degree as transformed cells expressing BRAF V600E in culture (PMID: 20538618).	20538618
BRAF T529M BRAF V600E	Advanced Solid Tumor	predicted - sensitive	RAF265	Preclinical	Actionable	In a preclinical study, RAF265 inhibited kinase activity in vitro, and downstream Erk phosphorylation in cells expressing BRAF V600E and the gatekeeper mutation BRAF T529M to a similar degree as transformed cells expressing BRAF V600E in culture (PMID: 20538618).	20538618
BRAF T529N BRAF V600E	Advanced Solid Tumor	resistant	RAF265	Preclinical	Actionable	In a preclinical study, transformed cells expressing BRAF V600E and the gatepkeeper mutation BRAF T529N were insensitive to RAF265 in culture (PMID: 20538618).	20538618
BRAF V600E	Advanced Solid Tumor	sensitive	RAF265	Preclinical	Actionable	In a preclinical study, RAF265 inhibited Erk phosphorylation and cell proliferation in BRAF V600E expressing cells in culture (PMID: 20538618).	20538618
BRAF wild-type	melanoma	predicted - sensitive	RAF265	Preclinical	Actionable	In a preclinical study, RAF265 inhibited the growth of melanoma tumors orthotopically implanted in mice, including tumors wild-type for BRAF (PMID: 22351689).	22351689

Showing 1 to 10 of 10 entries

Filter rows:

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.

Filter rows:

Showing 0 to 0 of 0 entries

Showing 0 to 0 of 0 entries

Filter rows:

Additional content available in CKB BOOST