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Key Documents

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SML3126

Sigma-Aldrich

BI-2852

≥98% (HPLC)

Sinónimos:

(3S)-2,3-Dihydro-5-hydroxy-3-[2-[[[[1-[(1-methyl-1H-imidazol-4-yl)methyl]-1H-indol-6-yl]methyl]amino]methyl]-1H-indol-3-yl]-1H-isoindol-1-one, (S)-5-Hydroxy-3-(2-(((1-((1-methyl-1H-imidazol-4-yl)methyl)-1H-indol-6-yl)methylamino)methyl)-1H-indol-3-yl)isoindolin-1-one, BI 2852, BI2852

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About This Item

Fórmula empírica (notación de Hill):
C31H28N6O2
Número de CAS:
2375482-51-0
Peso molecular:
516.59
MDL number:
MFCD32197229
UNSPSC Code:
12352200
NACRES:
NA.77

Quality Level

100

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

2-8°C

SMILES string

O=C1C2=C([C@H](N1)C3=C(NC4=C3C=CC=C4)CNCC5=CC6=C(C=C5)C=CN6CC7=CN(C=N7)C)C=C(C=C2)O

Biochem/physiol Actions

BI-2852 is RAS inhibitor that binds RAS switch I and II (SI/II) pocket in both the active and inactive forms (GCP-/GDP-bound KD in μM = 0.74/2.0 (KRAS-G12D), 7.5/1.1 (KRAS), 0.57/2.5 (HRAS), 1.3/8.3 (NRAS)). BI-2852 inhibits RAS-mediated signaling and proliferation of KRAS-G12C-bearing NCI-H358 lung cancer cells (EGF-induced pERK IC50 = 5.8 μM; GI50 = 6.7 μM in soft agar with low serum) by blocking KRAS interactions with GEF SOS1 (GDP-bound G12C/G12D IC50 = 450/260 nM, GTP-bound Wt/G12C/G12D IC50 = 490/360/490 nM) and effectors CRAF (GTP-bound Wt/G12C/G12D IC50 = 1740/80/770 nM) and PI3Kα (GTP-bound Wt/G12C/G12D IC50 = 250/100/500 nM).

Storage Class

11 - Combustible Solids

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificados de análisis (COA)

Busque Certificados de análisis (COA) introduciendo el número de lote del producto. Los números de lote se encuentran en la etiqueta del producto después de las palabras «Lot» o «Batch»

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Dirk Kessler et al.
Proceedings of the National Academy of Sciences of the United States of America, 116(32), 15823-15829 (2019-07-25)
The 3 human RAS genes, KRAS, NRAS, and HRAS, encode 4 different RAS proteins which belong to the protein family of small GTPases that function as binary molecular switches involved in cell signaling. Activating mutations in RAS are among the
The small molecule BI-2852 induces a nonfunctional dimer of KRAS.
Timothy H Tran et al.
Proceedings of the National Academy of Sciences of the United States of America, 117(7), 3363-3364 (2020-02-13)
Reply to Tran et al.: Dimeric KRAS protein-protein interaction stabilizers.
Dirk Kessler et al.
Proceedings of the National Academy of Sciences of the United States of America, 117(7), 3365-3367 (2020-02-13)
Rachel Cooley et al.
Wellcome open research, 5, 20-20 (2020-06-27)
Targeting the interaction of proteins with weak binding affinities or low solubility represents a particular challenge for drug screening. The NanoLuc â ® Binary Technology (NanoBiT â ®) was originally developed to detect protein-protein interactions in live mammalian cells. Here we report

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