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SML3126

BI-2852

≥98% (HPLC)

Synonym(s):

(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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Size/SKUAvailabilityPrice
5 mg
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$371.00
25 mg

Available to ship TODAYfromMILWAUKEE

$1,480.00

About This Item

Empirical Formula (Hill Notation):
C31H28N6O2
CAS Number:
Molecular Weight:
516.59
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
Assay:
≥98% (HPLC)
Form:
powder

$371.00


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Quality Segment

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

InChI key

JYEQLXOWWLNVDX-PMERELPUSA-N

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

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This Item
SML03461642212SML0084
description

≥98% (HPLC)

description

≥98% (HPLC)

description

United States Pharmacopeia (USP) Reference Standard

description

≥98% (HPLC)

form

powder

form

powder

form

-

form

powder

assay

≥98% (HPLC)

assay

≥98% (HPLC)

assay

-

assay

≥98% (HPLC)

Quality Level

100

Quality Level

100

Quality Level

-

Quality Level

100

storage temp.

2-8°C

storage temp.

2-8°C

storage temp.

−20°C

storage temp.

2-8°C

solubility

DMSO: 2 mg/mL, clear

solubility

H2O: ≥5 mg/mL at warmed

solubility

-

solubility

DMSO: ≥9 mg/mL

color

white to beige

color

white to beige

color

-

color

yellow-orange


Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable



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