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SML3055

Sigma-Aldrich

LY3009120

≥98% (HPLC)

Synonym(s):

1-(3,3-Dimethylbutyl)-3-(2-fluoro-4-methyl-5-(7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)urea, DP 4978, DP-4978, DP4978, LY 3009120, LY-3009120, N-(3,3-Dimethylbutyl)-N′-[2-fluoro-4-methyl-5-[7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl]phenyl]urea

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About This Item

Empirical Formula (Hill Notation):
C23H29FN6O
CAS Number:
1454682-72-4
Molecular Weight:
424.51
MDL number:
MFCD28411374
UNSPSC Code:
12352200
NACRES:
NA.77

Quality Level

100

Assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear (warmed)

storage temp.

2-8°C

SMILES string

CC1=CC(F)=C(C=C1C2=C(N=C3N=C(N=CC3=C2)NC)C)NC(NCCC(C)(C)C)=O

InChI

1S/C23H29FN6O/c1-13-9-18(24)19(29-22(31)26-8-7-23(3,4)5)11-16(13)17-10-15-12-27-21(25-6)30-20(15)28-14(17)2/h9-12H,7-8H2,1-6H3,(H2,26,29,31)(H,25,27,28,30)

InChI key

HHCBMISMPSAZBF-UHFFFAOYSA-N

Biochem/physiol Actions

LY3009120 is an orally active, potent and selective pan-RAF type II inhibitor (IC50 = 4.3 nM/CRAF (c-Raf, Raf-1), 5.8 nM/BRAF(V600E), 15 nM/BRAF (b-Raf) by kinase assay with 1 mM ATP; IC50 = 44 nM/ARAF, 31-47 nM/BRAF, 42 nM/CRAF, >1 μM/155 other kinases by cell-based KiNativ affinity binding assay). LY3009120 inhibits RAF-dependent proliferation in cancer cultures (A375/HCT116 IC50 = 9.2/220 nM) and exhibits anti-tumor efficacy in a rat BRAF V600E ST019VR PDX model in vivo (15-30 mg/kg b.i.d. p.o.).

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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Wei-Jun Wei et al.
Theranostics, 7(4), 987-1001 (2017-04-07)
Although the prognosis of differentiated thyroid cancer (DTC) is relatively good, 30-40% of patients with distant metastases develop resistance to radioactive iodine therapy due to tumor dedifferentiation. For DTC patients harboring BRAFV600E mutation, Vemurafenib, a BRAF kinase inhibitor, has dramatically
Shih-Hsun Chen et al.
Cancer discovery, 6(3), 300-315 (2016-01-07)
We have identified previously undiscovered BRAF in-frame deletions near the αC-helix region of the kinase domain in pancreatic, lung, ovarian, and thyroid cancers. These deletions are mutually exclusive with KRAS mutations and occur in 4.21% of KRAS wild-type pancreatic cancer.
S-H Chen et al.
Oncogene, 37(6), 821-832 (2017-10-24)
KRAS, NRAS and BRAF mutations are among the most important oncogenic drivers in many major cancer types, such as melanoma, lung, colorectal and pancreatic cancer. There is currently no effective therapy for the treatment of RAS mutant cancers. LY3009120, a
Sheng-Bin Peng et al.
Cancer cell, 28(3), 384-398 (2015-09-08)
LY3009120 is a pan-RAF and RAF dimer inhibitor that inhibits all RAF isoforms and occupies both protomers in RAF dimers. Biochemical and cellular analyses revealed that LY3009120 inhibits ARAF, BRAF, and CRAF isoforms with similar affinity, while vemurafenib or dabrafenib
James R Henry et al.
Journal of medicinal chemistry, 58(10), 4165-4179 (2015-05-13)
The RAS-RAF-MEK-MAPK cascade is an essential signaling pathway, with activation typically mediated through cell surface receptors. The kinase inhibitors vemurafenib and dabrafenib, which target oncogenic BRAF V600E, have shown significant clinical efficacy in melanoma patients harboring this mutation. Because of
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