[CAS NO. 2375482-51-0] BI-2852

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PRODUCTS SPECIFICATIONS [2375482-51-0]

Catalog

HY-126247

Brand

MCE

CAS

2375482-51-0

DESCRIPTION [2375482-51-0]

Overview

MDL	-
Molecular Weight	516.59
Molecular Formula	C31H28N6O2
SMILES	OC(C=C1)=CC([C@@H](C2=C(CNCC3=CC4=C(C=CN4CC5=CN(C)C=N5)C=C3)NC6=CC=CC=C62)N7)=C1C7=O

For research use only. We do not sell to patients.

Summary

BI-2852 is a KRAS inhibitor for the switch I/II pocket (SI/II-pocket) by structure-based drug design with nanomolar affinity. BI-2852 is mechanistically distinct from covalent KRAS ^G12C inhibitor (binds to switch II pocket) and binds ten-fold more strongly to active KRAS ^G12D versus KRAS ^wt (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 ^[1] .

IC50 & Target

KRAS(G12C)

450 nM (IC ₅₀ )

KRAS(G12C)

750 nM (Kd)

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 ^[1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, stored under nitrogen

* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility

In Vitro:

DMSO : 55 mg/mL ( 106.47 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.9358 mL	9.6789 mL	19.3577 mL
5 mM	0.3872 mL	1.9358 mL	3.8715 mL
10 mM	0.1936 mL	0.9679 mL	1.9358 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.5 mg/mL (4.84 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (4.84 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.5 mg/mL (4.84 mM); Clear solution

* All of the co-solvents are available by MCE.