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Cat. No.: HY-164492

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LSN3074753

LSN3074753, an analog of LY3009120 (HY-12558), is a pan-RAF and Raf dimer inhibitor. LSN3074753 demonstrates activity against tumor cells with MAPK pathway activation driven by BRAF monomer or RAF dimers including BRAF- or KRAS-mutant colorectal cancer. LSN3074753 combined with Cetuximab (HY-P9905) shows additive and synergistic effects for colorectal cancer PDX models, particularly those with KRAS or BRAF mutation.

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CAS No.: 1455031-68-1
화학식: C₂₄H₃₀FN₅O₂
분자량:439.53

보관:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (266 KB)

LSN3074753 Chemical Structure

CAS No.: 1455031-68-1

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Use of MCE Products

Fluorescent Dye

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

Biological Activity
- 제품 설명
- Cellular Effect
Chemical Information
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

All Raf Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A-375	ED₅₀	1.7 mg/kg Compound: 6	In vivo inhibition of BRAF V600E mutant in human A375 cells xenografted in po dosed athymic nu/nu mouse assessed as inhibition of ERK phosphorylation by ELISA In vivo inhibition of BRAF V600E mutant in human A375 cells xenografted in po dosed athymic nu/nu mouse assessed as inhibition of ERK phosphorylation by ELISA	[PMID: 25965804]
A-375	IC₅₀	0.01 μM Compound: 6	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	0.022 μM Compound: 6	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]
HCT-116	IC₅₀	0.16 μM Compound: 6	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	0.174 μM Compound: 6	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]

Chemical Information

CAS No. 1455031-68-1
분자량 439.53
화학식 C₂₄H₃₀FN₅O₂
SMILES

O=C(NC[C@@H](O)C(C)(C)C)NC1=CC(C2=CC3=CN=C(NC)C=C3N=C2C)=C(C)C=C1F
선적

Room temperature in continental US; may vary elsewhere.
보관

Please store the product under the recommended conditions in the Certificate of Analysis.

순도&문서

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (266 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)

References

[1]. Yao YM, et al. Mouse PDX Trial Suggests Synergy of Concurrent Inhibition of RAF and EGFR in Colorectal Cancer with BRAF or KRAS Mutations. Clin Cancer Res. 2017 Sep 15;23(18):5547-5560. [Content Brief]

[2]. Sorokin A, et al. Antitumor activity of panRAF inhibition in BRAF V600E metastatic colorectal cancer[J]. 2017.

Calculators

몰농도 계산기

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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.

Keywords

MOQ

Minimum order quantity

100 mg

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Biological Activity
- 제품 설명
Chemical Information
순도&문서
References

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LSN3074753

All Raf Isoforms

Biological Activity

Chemical Information

순도&문서

References

Calculators

Help & FAQs

LSN3074753 Related Classifications

HY-164492 Related Classifications