GLPBio

(R)-BI-2852

Catalog No.: GC72968Purity:>97.00%
COASDSData Sheet
(R)-BI-2852 is the isomer of BI-2852 , and can be used as an experimental control.

Products are for research use only. Not for human use. We do not sell to patients.

(R)-BI-2852
Cas No.: 2375482-49-6
1 mgIn Stock
$108.00
1
5 mgIn Stock
$207.00
1
10 mgIn Stock
$324.00
1
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Description

(R)-BI-2852 is the isomer of BI-2852 , and can be used as an experimental control. 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.

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

Product Documents

Purity:>97.00%Appearance:A solid
COASDSData Sheet

Chemical Properties

CAS No.
2375482-49-6
Molecular Formula
C31H28N6O2
Molecular Weight
516.59
Solubility
DMSO : 55 mg/mL (106.47 mM; Need ultrasonic)
Storage
4°C, stored under nitrogen
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

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