Art. -Nr.: HY-12558

LY3009120

(Synonyms: DP-4978)

14 Cited Publications

Kundenbewertung

Based on 14 publication(s) in Google Scholar

LY3009120 (DP-4978) is a pan RAF inhibitor which inhibits BRAF^V600E, BRAF^WT and CRAF^WT with IC₅₀s of 5.8, 9.1 and 15 nM, respectively.

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Reinheit: 98.66%
CAS. Nr.: 1454682-72-4
Formel: C₂₃H₂₉FN₆O
Molecular Weight:424.51

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

LY3009120 Chemical Structure

CAS. Nr.: 1454682-72-4

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (14)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

LY3009120 (DP-4978) is a pan RAF inhibitor which inhibits BRAF^V600E, BRAF^WT and CRAF^WT with IC₅₀s of 5.8, 9.1 and 15 nM, respectively.

IC₅₀ & Target^[1]

BRaf^V600E

5.8 nM (IC₅₀)

Braf

9.1 nM (IC₅₀)

CRAF

15 nM (IC₅₀)

Alle Raf Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
A-375	EC₅₀	4.36 mg/kg Compound: 13, LY3009120	In vivo inhibition of BRAF V600E mutant in human A375 cells xenografted in po dosed NIH nude rat assessed as inhibition of ERK phosphorylation by ELISA In vivo inhibition of BRAF V600E mutant in human A375 cells xenografted in po dosed NIH nude rat assessed as inhibition of ERK phosphorylation by ELISA	[PMID: 25965804]
A-375	IC₅₀	0.0092 μM Compound: 13, LY3009120	Antiproliferative activity against human A375 cells after 72 hrs by resazurin assay Antiproliferative activity against human A375 cells after 72 hrs by resazurin assay	[PMID: 25965804]
A-375	IC₅₀	0.037 μM Compound: 13, LY3009120	Inhibition of BRAF V600E mutant in human A375 cells assessed as inhibition of ERK phosphorylation measured after 72 hrs by ELISA assay Inhibition of BRAF V600E mutant in human A375 cells assessed as inhibition of ERK phosphorylation measured after 72 hrs by ELISA assay	[PMID: 25965804]
A-375	IC₅₀	0.3 μM Compound: LY3009120	Antiproliferative activity against human A375 cells after 72 hrs by Cell-Titer Glo assay Antiproliferative activity against human A375 cells after 72 hrs by Cell-Titer Glo assay	[PMID: 30529543]
A-375	IC₅₀	100 nM Compound: 13, LY3009120	Competitive binding affinity to EphB4 in human A375 cells after 15 mins in presence of ATP analogue Competitive binding affinity to EphB4 in human A375 cells after 15 mins in presence of ATP analogue	[PMID: 25965804]
A-375	IC₅₀	20 nM Compound: 13, LY3009120	Competitive binding affinity to EphA2 in human A375 cells after 15 mins in presence of ATP analogue Competitive binding affinity to EphA2 in human A375 cells after 15 mins in presence of ATP analogue	[PMID: 25965804]
A-375	IC₅₀	28.3 nM Compound: 1; LY3009120	Antiproliferative activity against human A-375 cells harboring BRAF mutant assessed as reduction in cell viability incubated for 24 hrs by Click-iT EdU cell proliferation imaging assay Antiproliferative activity against human A-375 cells harboring BRAF mutant assessed as reduction in cell viability incubated for 24 hrs by Click-iT EdU cell proliferation imaging assay	[PMID: 33780623]
A-375	IC₅₀	28.3 nM Compound: 1; LY3009120	Antiproliferative activity against human A375 cells harboring BRAF mutant assessed as reduction in cell viability Antiproliferative activity against human A375 cells harboring BRAF mutant assessed as reduction in cell viability	[PMID: 34055227]
A-375	IC₅₀	290 nM Compound: 13, LY3009120	Competitive binding affinity to CSK in human A375 cells after 15 mins in presence of ATP analogue Competitive binding affinity to CSK in human A375 cells after 15 mins in presence of ATP analogue	[PMID: 25965804]
A-375	IC₅₀	31 nM Compound: 13, LY3009120	Competitive binding affinity to BRAF in human A375 cells after 15 mins in presence of ATP analogue Competitive binding affinity to BRAF in human A375 cells after 15 mins in presence of ATP analogue	[PMID: 25965804]
A-375	IC₅₀	310 nM Compound: 13, LY3009120	Competitive binding affinity to SRC in human A375 cells after 15 mins in presence of ATP analogue Competitive binding affinity to SRC in human A375 cells after 15 mins in presence of ATP analogue	[PMID: 25965804]
A-375	IC₅₀	380 nM Compound: 13, LY3009120	Competitive binding affinity to ABL in human A375 cells after 15 mins in presence of ATP analogue Competitive binding affinity to ABL in human A375 cells after 15 mins in presence of ATP analogue	[PMID: 25965804]
A-375	IC₅₀	39 nM Compound: 13, LY3009120	Competitive binding affinity to ZAK in human A375 cells after 15 mins in presence of ATP analogue Competitive binding affinity to ZAK in human A375 cells after 15 mins in presence of ATP analogue	[PMID: 25965804]
A-375	IC₅₀	390 nM Compound: 13, LY3009120	Competitive binding affinity to IRAK1 in human A375 cells after 15 mins in presence of ATP analogue Competitive binding affinity to IRAK1 in human A375 cells after 15 mins in presence of ATP analogue	[PMID: 25965804]
A-375	IC₅₀	42 nM Compound: 13, LY3009120	Competitive binding affinity to CRAF in human A375 cells after 15 mins in presence of ATP analogue Competitive binding affinity to CRAF in human A375 cells after 15 mins in presence of ATP analogue	[PMID: 25965804]
A-375	IC₅₀	44 nM Compound: 13, LY3009120	Competitive binding affinity to ARAF in human A375 cells after 15 mins in presence of ATP analogue Competitive binding affinity to ARAF in human A375 cells after 15 mins in presence of ATP analogue	[PMID: 25965804]
A-375	IC₅₀	450 nM Compound: 13, LY3009120	Competitive binding affinity to GCN2 in human A375 cells after 15 mins in presence of ATP analogue Competitive binding affinity to GCN2 in human A375 cells after 15 mins in presence of ATP analogue	[PMID: 25965804]
A-375	IC₅₀	470 nM Compound: 13, LY3009120	Competitive binding affinity to JNK in human A375 cells after 15 mins in presence of ATP analogue Competitive binding affinity to JNK in human A375 cells after 15 mins in presence of ATP analogue	[PMID: 25965804]
A-375	IC₅₀	61 nM Compound: 13, LY3009120	Competitive binding affinity to p38 in human A375 cells after 15 mins in presence of ATP analogue Competitive binding affinity to p38 in human A375 cells after 15 mins in presence of ATP analogue	[PMID: 25965804]
A-375	IC₅₀	800 nM Compound: 13, LY3009120	Competitive binding affinity to MAP2K5 in human A375 cells after 15 mins in presence of ATP analogue Competitive binding affinity to MAP2K5 in human A375 cells after 15 mins in presence of ATP analogue	[PMID: 25965804]
A-375	IC₅₀	91 nM Compound: 13, LY3009120	Competitive binding affinity to FYN in human A375 cells after 15 mins in presence of ATP analogue Competitive binding affinity to FYN in human A375 cells after 15 mins in presence of ATP analogue	[PMID: 25965804]
A-375	IC₅₀	970 nM Compound: 13, LY3009120	Competitive binding affinity to KHS1 in human A375 cells after 15 mins in presence of ATP analogue Competitive binding affinity to KHS1 in human A375 cells after 15 mins in presence of ATP analogue	[PMID: 25965804]
A-375	IC₅₀	98 nM Compound: 13, LY3009120	Competitive binding affinity to MAP3K1 in human A375 cells after 15 mins in presence of ATP analogue Competitive binding affinity to MAP3K1 in human A375 cells after 15 mins in presence of ATP analogue	[PMID: 25965804]
A549	IC₅₀	45.6 nM Compound: 1; LY3009120	Synergistic antiproliferative activity against human A549 cells harboring KRAS mutant assessed as reduction in cell viability incubated for 24 hrs in presence of 100 nM cobimetinib by Click-iT EdU cell proliferation imaging assay Synergistic antiproliferative activity against human A549 cells harboring KRAS mutant assessed as reduction in cell viability incubated for 24 hrs in presence of 100 nM cobimetinib by Click-iT EdU cell proliferation imaging assay	[PMID: 33780623]
A549	IC₅₀	45.6 nM Compound: 1; LY3009120	Synergistic antiproliferative activity against human A549 cells harboring KRAS mutant assessed as reduction in cell viability in presence of 100 nM cobi-metinib Synergistic antiproliferative activity against human A549 cells harboring KRAS mutant assessed as reduction in cell viability in presence of 100 nM cobi-metinib	[PMID: 34055227]
A549	IC₅₀	545 nM Compound: 1; LY3009120	Antiproliferative activity against human A549 cells harboring KRAS mutant assessed as reduction in cell viability incubated for 24 hrs by Click-iT EdU cell proliferation imaging assay Antiproliferative activity against human A549 cells harboring KRAS mutant assessed as reduction in cell viability incubated for 24 hrs by Click-iT EdU cell proliferation imaging assay	[PMID: 33780623]
A549	IC₅₀	545 nM Compound: 1; LY3009120	Antiproliferative activity against human A549 cells harboring KRAS mutant assessed as reduction in cell viability Antiproliferative activity against human A549 cells harboring KRAS mutant assessed as reduction in cell viability	[PMID: 34055227]
HCT-116	IC₅₀	0.15 μM Compound: 13, LY3009120	Inhibition of KRAS G13D mutant in human HCT116 cells assessed as inhibition of ERK phosphorylation by ELISA Inhibition of KRAS G13D mutant in human HCT116 cells assessed as inhibition of ERK phosphorylation by ELISA	[PMID: 25965804]
HCT-116	IC₅₀	0.22 μM Compound: 13, LY3009120	Antiproliferative activity against human HCT116 cells after 67 hrs by resazurin assay Antiproliferative activity against human HCT116 cells after 67 hrs by resazurin assay	[PMID: 25965804]
HepG2	IC₅₀	2.6 μM Compound: LY3009120	Antiproliferative activity against human HepG2 cells after 72 hrs by Cell-Titer Glo assay Antiproliferative activity against human HepG2 cells after 72 hrs by Cell-Titer Glo assay	[PMID: 30529543]
HT-29	IC₅₀	0.9 μM Compound: LY3009120	Antiproliferative activity against human HT-29 cells after 72 hrs by Cell-Titer Glo assay Antiproliferative activity against human HT-29 cells after 72 hrs by Cell-Titer Glo assay	[PMID: 30529543]
MV4-11	IC₅₀	0.1 μM Compound: LY3009120	Antiproliferative activity against human MV4-11 cells after 72 hrs by Cell-Titer Glo assay Antiproliferative activity against human MV4-11 cells after 72 hrs by Cell-Titer Glo assay	[PMID: 30529543]
SK-MEL-2	IC₅₀	0.2 μM Compound: LY3009120	Antiproliferative activity against human SK-MEL-2 cells after 72 hrs by Cell-Titer Glo assay Antiproliferative activity against human SK-MEL-2 cells after 72 hrs by Cell-Titer Glo assay	[PMID: 30529543]

In Vitro

In the whole-cell based KiNativ assay, LY3009120 shows affinity to each RAF isoform with the IC₅₀ of 44, 31-47 and 42 nM for ARAF, BRAF and CRAF respectively. LY3009120 exhibits anti-proliferative effects on cell lines harboring BRAF^V600E, KRAS^G13 and KRAS^G12 mutations. LY3009120 (1 μM) inhibits the phosphorylation of both MEK1/2 and ERK1/2 in cell lines with high basal levels of pMEK1/2 and pERK1/2 (RKO and HCT 116)^[1]. LY3009120 shows inhibitory effect on tumor cells such as BxPC-3, NCI-H2405 and OV-90 cell lines. LY3009120 (0.01 μM) demonstrates potent and dose-dependent inhibition of phospho-MEK and ERK in all three cell lines. LY3009120 demonstrates a concentration-dependent cell growth inhibition with IC₅₀ values of 0.04, 0.087, and 0.007 μM against H2405, BxPC-3, and OV-90 cells, respectively^[2]. LY3009120 inhibits BRAF^WT, CRAF^WT, BRAF^V600E, and BRAF^V600E+G468A with the IC₅₀ values of 9.1, 15, 5.8, and 17 nM, respectively. LY3009120 induces BRAF-CRAF dimerization but inhibits the phosphorylation of downstream MEK and ERK. LY3009120 also inhibits various forms of RAF dimers including BRAF or CRAF homodimers^[3]. LY3009120 gives only very minor activation at very low doses, with near complete inhibition of phospho-ERK at concentrations above 100 nM^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

LY3009120 (20 mg/kg bid) displays significant activity in in vivo BRAF^mut and KRAS^mut CRC xenograft models. In Colo 205 xenografts (BRAF^mut), LY3009120 results in statistically significant tumor regression, while treatment of HCT 116 xenografts (KRAS^mut) results in statistically significant inhibition of tumor growth. LY3009120 treatment reduces pMEK1/2 in all HT-29 xenografts and reduces pERK1/2 in the majority of HT-29 xenografts^[1]. LY3009120 (15 or 30 mg/kg) achieves almost complete tumor growth regression, and inhibits downstream phospho-MEK and ERK by approximately 70% and 60%, respectively, in the H2405 model^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 1454682-72-4
Appearance Solid
Molecular Weight 424.51
Formel C₂₃H₂₉FN₆O
Color Light yellow to khaki
SMILES

O=C(NC1=CC(C2=CC3=CN=C(NC)N=C3N=C2C)=C(C)C=C1F)NCCC(C)(C)C
Synonyms

DP-4978
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (14)

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Signal Transduct Target Ther

Tet methylcytosine dioxygenase 2 (TET2) deficiency elicits EGFR-TKI (tyrosine kinase inhibitors) resistance in non-small cell lung cancer. [Abstract]

2024 Mar 9;9(1):65. PMID: 38461173
Cancer Res

Activity and Resistance of a Brain-Permeable Paradox Breaker BRAF Inhibitor in Melanoma Brain Metastasis. [Abstract]

2022 Jul 18;82(14):2552-2564. PMID: 35584009
Oncogene

RAF1 facilitates KIT signaling and serves as a potential treatment target for gastrointestinal stromal tumor. [Abstract]

2024 May 17. PMID: 38760447
Oncogene

The dimer-dependent catalytic activity of RAF family kinases is revealed through characterizing their oncogenic mutants. [Abstract]

2018 Oct;37(43):5719-5734. PMID: 29930381

LY3009120 purchased from MedChemExpress. Usage Cited in: Oncogene. 2018 Oct;37(43):5719-5734. [Abstract]

BRAF mutants with in-frame β3-αC loop deletions have approximate sensitivities to RAF dimer inhibitor, LY3009120.
Cell Syst

Receptor-Driven ERK Pulses Reconfigure MAPK Signaling and Enable Persistence of Drug-Adapted BRAF-Mutant Melanoma Cells. [Abstract]

2020 Nov 18;11(5):478-494.e9. PMID: 33113355
Clin Sci (Lond)

A pan-RAF inhibitor LY3009120 inhibits necroptosis by preventing phosphorylation of RIPK1 and alleviates dextran sulfate sodium-induced colitis. [Abstract]

2019 Apr 16;133(8):919-932. PMID: 30944150

LY3009120 purchased from MedChemExpress. Usage Cited in: Clin Sci (Lond). 2019 Apr 16;133(8):919-932. [Abstract]

LY3009120 decreases phosphorylation of RIPK1, RIPK3 and MLKL in T/S/Z treated HT-29 cells. HT-29 cells are pretreated with DMSO or LY3009120 for 1 hour, then treated with T/S/Z for 0, 2, 4 and 6 hours, respectively.

LY3009120 purchased from MedChemExpress. Usage Cited in: Clin Sci (Lond). 2019 Apr 16;133(8):919-932. [Abstract]

Colonic proteins on day 7 are tested by immunoblotting to detect p-MLKL, MLKL and cleaved caspase-3 with corresponding antibodies. GAPDH is used as an internal control. Three individual mice from each group are shown.
Cancer Sci

Altered intracellular signaling by imatinib increases the anti-cancer effects of tyrosine kinase inhibitors in chronic myelogenous leukemia cells. [Abstract]

2018 Jan;109(1):121-131. PMID: 29121435
Neoplasia

STAMBP promotes lung adenocarcinoma metastasis by regulating the EGFR/MAPK signaling pathway. [Abstract]

2021 Jun;23(6):607-623. PMID: 34102455
J Biol Chem

Crosstalk between Protein Kinase C α and Transforming Growth Factor β Signaling Mediated by Runx2 in Intestinal Epithelial Cells. [Abstract]

2023 Apr;299(4):103017. PMID: 36791912
bioRxiv

2024 August 16.
Research Square Print

December 21st, 2022.
Research Square Print

October 27th, 2022.
bioRxiv

2019 Sep.
Methods Mol Biol

Methods for High-throughput Drug Combination Screening and Synergy Scoring. [Abstract]

2018:1711:351-398. PMID: 29344898

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 38 mg/mL (89.51 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.3557 mL

11.7783 mL

23.5566 mL

5 mM

0.4711 mL

2.3557 mL

4.7113 mL

10 mM

0.2356 mL

1.1778 mL

2.3557 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 5% DMSO 95% (20% SBE-β-CD in Saline)

Solubility: 2.5 mg/mL (5.89 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
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+
%
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The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protokoll

Cell Assay^[4]

Briefly, cells are grown in McCoy’s 5A supplemented with 10% characterized fetal bovine serum at 37°C, 5% CO₂, and 95% humidity. Cells are allowed to expand until 75-90% confluency at which point they are subcultured or harvested for assay use. A serial dilution of test compound is dispensed into a 384-well black clear bottom plate in triplicate. Six-hundred-twenty-five cells are added per well in 50 μL of complete growth medium in the 384-well plate. Plates are incubated for 67 h at 37°C, 5% CO₂, and 95% humidity. At the end of the incubation period, 10 μL of a 440 μM solution of resazurin in PBS is added to each well of the plate and plates are incubated for an additional 5 h at 37°C, 5% CO₂, and 95% humidity. Plates are read on a Synergy2 reader using an excitation of 540 nm and an emission of 600 nm. Data are analyzed using Prism softwareto calculate IC₅₀ values.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration^[2]

Briefly, 5×10⁶ to 10×10⁶ tumor cells in a 1:1 Matrigel mix (0.2 mL total volume) are injected subcutaneously into the right hind flank of female NIH nude rats. After tumors reach a desired size of approximately 300 mm³, animals are randomized into groups of 8 for efficacy studies. Drugs (LY3009120 or PLX4032) are administered orally (gavage) in 0.6-mL volume of vehicle with the dose schedules. Tumor growth and body weight are monitored over time to evaluate efficacy and signs of toxicity.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
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- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Vakana E, et al. LY3009120, a panRAF inhibitor, has significant anti-tumor activity in BRAF and KRAS mutant preclinical models of colorectal cancer. Oncotarget. 2017 Feb 7;8(6):9251-9266 [Content Brief]

[2]. Chen SH, et al. Oncogenic BRAF Deletions That Function as Homodimers and Are Sensitive to Inhibition by RAF Dimer Inhibitor LY3009120. Cancer Discov. 2016 Mar;6(3):300-15 [Content Brief]

[3]. Peng SB, et al. Inhibition of RAF Isoforms and Active Dimers by LY3009120 Leads to Anti-tumor Activities in RAS or BRAF Mutant Cancers. Cancer Cell. 2015 Sep 14;28(3):384-98 [Content Brief]

[4]. Henry JR, et al. Discovery of 1-(3,3-dimethylbutyl)-3-(2-fluoro-4-methyl-5-(7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)urea (LY3009120) as a pan-RAF inhibitor with minimal paradoxical activation and activity against BRAF or RAS mutant tumo [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.3557 mL	11.7783 mL	23.5566 mL	58.8914 mL
	5 mM	0.4711 mL	2.3557 mL	4.7113 mL	11.7783 mL
	10 mM	0.2356 mL	1.1778 mL	2.3557 mL	5.8891 mL
	15 mM	0.1570 mL	0.7852 mL	1.5704 mL	3.9261 mL
	20 mM	0.1178 mL	0.5889 mL	1.1778 mL	2.9446 mL
	25 mM	0.0942 mL	0.4711 mL	0.9423 mL	2.3557 mL
	30 mM	0.0785 mL	0.3926 mL	0.7852 mL	1.9630 mL
	40 mM	0.0589 mL	0.2945 mL	0.5889 mL	1.4723 mL
	50 mM	0.0471 mL	0.2356 mL	0.4711 mL	1.1778 mL
	60 mM	0.0393 mL	0.1963 mL	0.3926 mL	0.9815 mL
	80 mM	0.0294 mL	0.1472 mL	0.2945 mL	0.7361 mL

Keywords

LY3009120

14 Cited Publications

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LY3009120

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

MAPK Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Autophagy Compound Library

Oxygen Sensing Compound Library

Ferroptosis Compound Library

Glutamine Metabolism Compound Library

Anti-Pancreatic Cancer Compound Library

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Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

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Cell Death Library

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MCE Bioactive Compound Library

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Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) LY3009120

Alle Raf Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (14)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

LY3009120

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

MAPK Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Autophagy Compound Library

Oxygen Sensing Compound Library

Ferroptosis Compound Library

Glutamine Metabolism Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Obesity Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Heterocyclic Compound Library

Membrane Receptor-targeted Compound Library

Cell Death Library

Serine/Threonine Kinase Inhibitor Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Clinical Compound Library Plus

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) LY3009120

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