GDC-0879

For research use only.

Catalog No.S1104 Synonyms: AR-00341677

34 publications

GDC-0879 Chemical Structure

CAS No. 905281-76-7

GDC-0879 (AR-00341677) is a novel, potent, and selective B-Raf inhibitor with IC50 of 0.13 nM in A375 and Colo205 cells with activity against c-Raf as well; no inhibition known to other protein kinases.

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Selleck's GDC-0879 has been cited by 34 publications

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Biological Activity

Description GDC-0879 (AR-00341677) is a novel, potent, and selective B-Raf inhibitor with IC50 of 0.13 nM in A375 and Colo205 cells with activity against c-Raf as well; no inhibition known to other protein kinases.
Targets
B-Raf [1]
(A375, Colo205 cells)
0.13 nM
In vitro

GDC-0879 also inhibits cellular pERK with IC50 of 63 nM. GDC-0879 shows comparable potency in A375 melanoma and Colo205 colorectal carcinoma cell lines, both of which are B-RafV600E mutant, with IC50 of 59 nM and 29 nM for pMEK1 inhibition respectively. GDC-0879 potently inhibits B-RafV600E in Malme3M cells with IC50 of 0.75 μM. GDC-0879 also shows EC50 values < 0.5 μM in many tumor cells (A375, 624, SK-MEL-28, Malme3M, C32, 928, 888, G-361, Colo205, Colo206, SW1417, CL34, and Colo201). [1]
Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human MALME3M cells NHnKUWhHfW6ldHnvckBie3OjeR?= MX;Jcohq[mm2aX;uJI9nKEWUS{GvNkBxcG:|cHjvdplt[XSrb36gbY4hcHWvYX6gUWFNVUV|TTDj[YxteyxiSVO1NF0xNjB4MzFOwG0> NUHjOVVWOTF5MUewNFE>
human A375 cells MlXtVJJwdGmoZYLheIlwdiCjc4PhfS=> NEPNWJlCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFGzO|Uh[2WubIOg[ZhxemW|c3nu[{BDNVKjZjDWOlAxTSCvdYThcpQh[W6mIIfpcIQhfHmyZTDSZZMtKEmFNUC9NE42KM7:TR?= NX3xW4FpOjJ6MEi5NVE>
human A375 cells MX7GeY5kfGmxbjDhd5NigQ>? MljGTY5pcWKrdHnvckBw\iCkLWLh[kBqdiCqdX3hckBCOzd3IHPlcIx{KGG|c3Xzd4VlKHCqb4PwbI9zgWyjdHnvckBw\iCHUlusJGlEPTB;MTFOwG0> NEDyRVYzOjhyOEmxNS=>

... Click to View More Cell Line Experimental Data
In vivo In GDC-0879 treated mice, both cell line- and patient-derived BRAFV600E tumors exhibit stronger and more sustained pharmacodynamic inhibition (>90% for 8 hours) and improved survival compared to mutant KRAS-expressing tumors. Although there is involvement of activated RAF signaling in RAS-induced tumorigenesis, decreased time to progression is observed for some KRAS-mutant tumors following GDC-0879 administration. Whereas GDC-0879-mediated efficacy is associated strictly with B-RafV600E status, MEK inhibition also attenuates proliferation and tumor growth of cell lines expressing wild-type BRAF (81% KRAS mutant, 38% KRAS wild type). The responsiveness of B-RafV600E melanoma cells to GDC-0879 could be dramatically altered by pharmacologic and genetic modulation of PI3K pathway activity. [2]

Protocol

Animal Research:[2]
- Collapse
  • Animal Models: Female nu/nu mice
  • Dosages: 100 mg/kg
  • Administration: Oral gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 66 mg/mL warmed (197.38 mM)
Ethanol 5 mg/mL (14.95 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
0.5% methylcellulose+0.2% Tween 80
For best results, use promptly after mixing. 		30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 334.37
Formula

C19H18N4O2
CAS No. 905281-76-7
Storage powder
in solvent
Synonyms AR-00341677
Smiles C1CC(=NO)C2=C1C=C(C=C2)C3=CN(N=C3C4=CC=NC=C4)CCO

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID