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Dokumente

SML3055

Sigma-Aldrich

LY3009120

≥98% (HPLC)

Synonym(e):

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

Empirische Formel (Hill-System):
C23H29FN6O
CAS-Nummer:
1454682-72-4
Molekulargewicht:
424.51
MDL-Nummer:
MFCD28411374
UNSPSC-Code:
12352200
NACRES:
NA.77

Qualitätsniveau

100

Assay

≥98% (HPLC)

Form

powder

Farbe

white to beige

Löslichkeit

DMSO: 2 mg/mL, clear (warmed)

Lagertemp.

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)

InChIKey

HHCBMISMPSAZBF-UHFFFAOYSA-N

Biochem./physiol. Wirkung

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.).

Lagerklassenschlüssel

11 - Combustible Solids

WGK

WGK 3

Flammpunkt (°F)

Not applicable

Flammpunkt (°C)

Not applicable

Analysenzertifikate (COA)

Suchen Sie nach Analysenzertifikate (COA), indem Sie die Lot-/Chargennummer des Produkts eingeben. Lot- und Chargennummern sind auf dem Produktetikett hinter den Wörtern ‘Lot’ oder ‘Batch’ (Lot oder Charge) zu finden.

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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.
Su-Min Yang et al.
International journal of molecular medicine, 42(6), 3477-3484 (2018-10-03)
Excessive preadipocyte differentiation/adipogenesis is closely linked to the development of obesity. LY3009120 is a pan‑Raf kinase inhibitor and is known for its anticancer activities. In the present study, the effect of LY3009120 on 3T3‑L1 cell adipogenesis was investigated. The differentiation
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
Young B Kim et al.
Archives of biochemistry and biophysics, 445(1), 9-18 (2005-12-21)
Dipeptidyl peptidase-IV (DPP-IV) is a serine protease with a signature Asp-His-Ser motif at the active site. Our pH data suggest that Gly-Pro-pNA cleavage catalyzed by DPP-IV is facilitated by an ionization of a residue with a pK of 7.2 +/-
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