ChemicalBook > CAS DataBase List > BI-2852

BI-2852

Product Name
BI-2852
CAS No.
2375482-51-0
Chemical Name
BI-2852
Synonyms
BI-2852;BI-2852, 10 mM in DMSO;BI-2852,Ras,inhibit,BI 2852,Inhibitor,BI2852;(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;1H-Isoindol-1-one, 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]-, (3S)-
CBNumber
CB45430811
Molecular Formula
C31H28N6O2
Formula Weight
516.59
MOL File
2375482-51-0.mol
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BI-2852 Property

Boiling point:
906.5±65.0 °C(Predicted)
Density 
1.41±0.1 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
DMSO:77.5(Max Conc. mg/mL);150.02(Max Conc. mM)
Ethanol:23.0(Max Conc. mg/mL);44.52(Max Conc. mM)
form 
Solid
pka
8.95±0.40(Predicted)
color 
Off-white to light yellow
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
SML3126
Product name
BI-2852
Purity
≥98% (HPLC)
Packaging
5MG
Price
$346
Updated
2025/07/31
Sigma-Aldrich
Product number
SML3126
Product name
BI-2852
Purity
≥98% (HPLC)
Packaging
25MG
Price
$1380
Updated
2025/07/31
ChemScene
Product number
CS-0100975
Product name
BI-2852
Purity
98.74%
Packaging
50mg
Price
$1650
Updated
2021/12/16
ChemScene
Product number
CS-0100975
Product name
BI-2852
Purity
98.74%
Packaging
100mg
Price
$2900
Updated
2021/12/16
ChemScene
Product number
CS-0100975
Product name
BI-2852
Purity
98.74%
Packaging
5mg
Price
$350
Updated
2021/12/16
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BI-2852 Chemical Properties,Usage,Production

Uses

BI-2852 is a KRAS inhibitor for the switch I/II pocket (SI/II-pocket) by structure-based agent design with nanomolar affinity. BI-2852 is mechanistically distinct from covalent KRASG12C inhibitor (binds to switch II pocket) and binds ten-fold more strongly to active KRASG12D versus KRASwt (740 nM vs 7.5 μM). BI-2852 blocks GEF, GAP, and effector interactions with KRAS, leading to inhibition of downstream signaling and an antiproliferative effect in KRAS mutant cells.

Biological Activity

BI-2852 is a switch SI/II pocket KRAS inhibitor with nanomolar affinity through structure-based drug design. It is mechanistically distinct from covalent KRASG12C inhibitors (binding switch II), binding to active KRASG12D 10-fold more strongly than KRAS wt (740 nM vs 7.5 μM). BI-2852 blocks GEF, GAP and effector interactions with KRAS, resulting in inhibition of downstream signaling and antiproliferative effects in KRAS mutant cells.

in vitro

BI-2852 (Compound 1) (10 nM-10 μM; 2 hours) shows a dose-dependent pERK modulation and antiproliferative effect at EC 50 s of 5.8 μM and 6.7 μM in soft agar and low serum conditions in NCI-H358 cells.

target

KRAS(G12C)

450 nM (IC 50 )

KRAS(G12C)

< p> 750 nM (Kd)

IC 50

KRAS(G12C): 450 nM (IC50); KRAS(G12C): 750 nM (Kd)

References

[1] Kessler D, et al. Drugging an undruggable pocket on KRAS. Proc Natl Acad Sci U S A. 2019 Aug 6; 116(32):15823-15829. DOI:10.1073/pnas.1904529116
[2] Dirk Kessler, et al. Drugging all RAS isoforms with one pocket. FUTURE MEDICINAL CHEMISTRY

BI-2852 Preparation Products And Raw materials

Raw materials

Preparation Products

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BI-2852 Suppliers

China 38 United States 5 Global 43
Chembest Research Laboratories Limited
Tel
+86-21-20908456
Fax
021-58180499
Email
sales@BioChemBest.com
Country
China
ProdList
6003
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61
BOC Sciences
Tel
1-631-485-4226; 16314854226
Email
info@bocsci.com
Country
United States
ProdList
12952
Advantage
65
ShangHai Caerulum Pharma Discovery Co., Ltd.
Tel
18149758185
Email
sales-cpd@caerulumpharma.com
Country
China
ProdList
3506
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58
Shanghai YuanQi Biotechnology Co., Ltd.
Tel
+86-2332782371 +86-18120098618
Email
sales@adobechem.com
Country
China
ProdList
1250
Advantage
50
Shanghai Lollane Biological Technology Co.,Ltd.
Tel
021-52996696，15000506266 15000506266
Fax
+86-21-52996696
Country
China
ProdList
4757
Advantage
55
ShangHai Biochempartner Co.,Ltd
Tel
177-54423994 17754423994
Fax
QQ:2853530913
Email
2853530910@QQ.com
Country
China
ProdList
8000
Advantage
62
TargetMol Chemicals Inc.
Tel
+1-781-999-5354; +17819995354
Email
marketing@targetmol.com
Country
United States
ProdList
32435
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58
ChemeGen(Shanghai) Biotechnology Co.,Ltd.
Tel
18818260767
Fax
QQ 3610331285
Email
sales@chemegen.com
Country
China
ProdList
11218
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58
Shanghai hongqu biomedical technology co. LTD
Tel
88888888888
Email
hongquchem@qq.com
Country
China
ProdList
5132
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58
Shanghai Sunmonth Technology Co., LTD
Tel
15216675652
Email
xuanyuelj@163.com
Country
China
ProdList
2864
Advantage
58

2375482-51-0, BI-2852Related Search:

DEMETON S METHYLERGONOVINE RMC-9805 RMC-7977 2-Propen-1-one, 1-[(3S)-4-[(7R)-7-[6-amino-4-methyl-3-(trifluoromethyl)-2-pyridinyl]-6-chloro-8-fluoro-2-[[(2S)-1-methyl-2-pyrrolidinyl]methoxy]-4-quinazolinyl]-3-methyl-1-piperazinyl]- MRTX1133 BI-2493 BI-2865

  • (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
  • 1H-Isoindol-1-one, 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]-, (3S)-
  • BI-2852,Ras,inhibit,BI 2852,Inhibitor,BI2852
  • BI-2852, 10 mM in DMSO
  • 2375482-51-0