BI-2852 free base · Synonyms: BI 2852 · BI2852

BI-2852 is a KRAS inhibitor.

For research use only. Not for human or veterinary use.

Target Ras

Research area Cancer

Purity 98+% Stock Inquire

Data Sheet SDS COA

BI-2852 structure

CAS No.: 2375482-51-0

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
100 mg	USD 598.00	BP-02356-100mg	In stock	Get quote
250 mg	USD 998.00	BP-02356-250mg	In stock	Get quote
500 mg	USD 1,788.00	BP-02356-500mg	In stock	Get quote
1 g	USD 2,980.00	BP-02356-1g	In stock	Get quote
2 g	Inquire	BP-02356-2g	In stock	Inquire

Need another size or custom synthesis? Request a quote.

Description

BI-2852 is a KRAS inhibitor for the switch I/II pocket (SI/II-pocket) by structure-based drug design with nanomolar affinity.

Biological activity

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) 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.

Identifiers

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
InChIKey: JYEQLXOWWLNVDX-PMERELPUSA-N

Specifications

MW (average): 516.5930
Formula: C₃₁H₂₈N₆O₂
CAS No.: 2375482-51-0
Physical state: Solid
Color: Off-white to light yellow
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO

In vitro: DMSO : 55 mg/mL

Documents

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

Same target

Search Ras

Same research area

Search Cancer