BI-2865( —— )

Catalog No. M29653 CAS No. 2937327-93-8

COA

Datasheet

HNMR

HPLC

MSDS

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Product Name

BI-2865
Note

Research use only, not for human use.
Brief Description

BI-2865 is a none-covalent pan-KRAS Inhibitor. BI-2865 binds to WT, G12C, G12D, G12V and G13D mutant KRAS with KDs of 6.9, 4.5, 32, 26, 4.3 nM respectively.
Description

BI-2865 is a none-covalent pan-KRAS Inhibitor. BI-2865 binds to WT, G12C, G12D, G12V and G13D mutant KRAS with KDs of 6.9, 4.5, 32, 26, 4.3 nM respectively. BI-2865 inhibits the proliferation of G12C, G12D or G12V mutant KRAS expressing BaF3 cells (mean IC50: roughly 140 nM).BI-2865 is a derivative with a prolinol substituent and a pyrimidine linker. BI-2865 has direct ionic interaction with E62, and a water-mediated hydrogen bond network with the side chain of R68 and the main chain carbonyl of Q61, as shown in Co-crystal structures of BI-2865 bound to KRAS.BI-2865 (5 days) inhibits the proliferation of G12C, G12D or G12V mutant KRAS expressing BaF3 cells in the presence of IL-13, with a mean IC50 of roughly 140?nM.
In Vitro

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In Vivo

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Synonyms

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Pathway

MAPK/ERK Signaling
Target

p38 MAPK
Recptor

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Research Area

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Indication

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CAS Number

2937327-93-8
Formula Weight

465.57
Molecular Formula

C23H27N7O2S
Purity

>98% (HPLC)
Solubility

DMSO : 250 mg/mL (536.98 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
SMILES

N#CC1=C(N)SC2=C1[C@@](C)(C3=NC(C4=NC(O[C@@H](C)[C@@H]5CCCN5C)=CC=N4)=NO3)CCC2
Chemical Name

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1. Kim D, et al. Pan-KRAS inhibitor disables oncogenic signalling and tumour growth. Nature. 2023 May 31.

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