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Merck
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주요 문서

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SML3126

Sigma-Aldrich

BI-2852

≥98% (HPLC)

동의어(들):

(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

실험식(Hill 표기법):
C31H28N6O2
CAS Number:
2375482-51-0
Molecular Weight:
516.59
MDL number:
MFCD32197229
UNSPSC 코드:
12352200
NACRES:
NA.77

Quality Level

100

분석

≥98% (HPLC)

양식

powder

색상

white to beige

solubility

DMSO: 2 mg/mL, clear

저장 온도

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

InChI key

JYEQLXOWWLNVDX-PMERELPUSA-N

생화학적/생리학적 작용

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).
RAS switch I and II (SI/II) pocket-targeting inhibitor against RAS-mediated signaling and proliferation by blocking KRAS interactions with GEF and effectors.

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point (°F)

Not applicable

Flash Point (°C)

Not applicable

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시험 성적서(COA)

Lot/Batch Number

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문서 라이브러리 방문

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)

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