BI-2852


Catalog No. Size PriceQuantity
M13816-2 2mg solid $200
M13816-10 10mg solid $695

Description

BI-2852 is a potent inhibitor of KRAS that binds with nanomolar affinity to a pocket between switch I and II on RAS. BI-2852 blocks all GEF, GAP, and effector interactions with KRAS, leading to inhibition of downstream signaling and an antiproliferative effect in the low micromolar range in KRAS mutant cells.

Product information

CAS Number: 2375482-51-0

Molecular Weight: 516.59

Formula: C31H28N6O2

Chemical Name: 5-hydroxy-3-(2-{[({1-[(1-methyl-1H-imidazol-4-yl)methyl]-1H-indol-6-yl}methyl)amino]methyl}-1H-indol-3-yl)-2,3-dihydro-1H-isoindol-1-one

Smiles: CN1C=NC(CN2C=CC3C=CC(CNCC4NC5=CC=CC=C5C=4C4NC(=O)C5C=CC(O)=CC=54)=CC2=3)=C1

InChiKey: JYEQLXOWWLNVDX-UHFFFAOYSA-N

InChi: InChI=1S/C31H28N6O2/c1-36-16-21(33-18-36)17-37-11-10-20-7-6-19(12-28(20)37)14-32-15-27-29(24-4-2-3-5-26(24)34-27)30-25-13-22(38)8-9-23(25)31(39)35-30/h2-13,16,18,30,32,34,38H,14-15,17H2,1H3,(H,35,39)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Solubility (25°C). 100 mg/mL(193.57 mM). Insoluble.

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

BI-2852 is a KRAS inhibitor that binds with nanomolar affinity to a pocket, thus far perceived to be “undruggable,” between switch I and II on RAS. BI-2852 is mechanistically distinct from covalent KRASG12C inhibitors because it binds to a different pocket present in both the active and inactive forms of KRAS. In doing so, it blocks all GEF, GAP, and effector interactions with KRAS, leading to inhibition of downstream signaling and an antiproliferative effect in the low micromolar range in KRAS mutant cells.

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.
  2. Dirk Kessler, et al. Drugging all RAS isoforms with one pocket. FUTURE MEDICINAL CHEMISTRY

Products are for research use only. Not for human use.

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