1. GPCR/G Protein
  2. Ras
  3. BI-2852

BI-2852 

Cat. No.: HY-126247 Purity: 98.02% ee.: 100.00%
Handling Instructions

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 KRASG12C inhibitor (binds to switch II pocket) because it binds to a different pocket present in both the active and inactive forms of KRAS. BI-2852 blocks GEF, GAP, and effector interactions with KRAS, leading to inhibition of downstream signaling and an antiproliferative effect in KRAS mutant cells.

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

BI-2852 Chemical Structure

BI-2852 Chemical Structure

CAS No. : 2375482-51-0

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 398 In-stock
Estimated Time of Arrival: December 31
5 mg USD 350 In-stock
Estimated Time of Arrival: December 31
10 mg USD 550 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1650 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2900 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

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 KRASG12C inhibitor (binds to switch II pocket) because it binds to a different pocket present in both the active and inactive forms of KRAS. 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[1]

KRAS(G12C)

450 nM (IC50)

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 EC50s of 5.8 µM and 6.7 µM in soft agar and low serum conditions in NCI-H358 cells[1].

Molecular Weight

516.59

Formula

C₃₁H₂₈N₆O₂

CAS No.

2375482-51-0

SMILES

OC(C=C1)=CC([[email protected]@H](C2=C(CNCC3=CC4=C(C=CN4CC5=CN(C)C=N5)C=C3)NC6=CC=CC=C62)N7)=C1C7=O

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)

References
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Keywords:

BI-2852BI2852BI 2852RasInhibitorinhibitorinhibit

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BI-2852
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