Key Documents

BI-2865

Name: BI-2865
Brand: SIGMA

≥98% (HPLC), powder

Synonym(s):

(4S)-2-Amino-4,5,6,7-tetrahydro-4-methyl-4-[3-[4-[(1S)-1-[(2S)-1-methyl-2-pyrrolidinyl]ethoxy]-2-pyrimidinyl]-1,2,4-oxadiazol-5-yl]- benzo[b]thiophene-3-carbonitrile, (S)-2-amino-4-methyl-4-(3-(4-((S)-1-((S)-1-methylpyrrolidin-2-yl)ethoxy)pyrimidin-2-yl)-1,2,4-oxadiazol-5-yl)-4,5,6,7-tetrahydrobenzo[b]thiophene-3-carbonitrile

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About This Item

Empirical Formula (Hill Notation):

C₂₃H₂₇N₇O₂S

CAS Number:

2937327-93-8

Molecular Weight:

465.57

MDL number:

MFCD35067897

NACRES:

NA.21

Assay:

≥98% (HPLC)

Form:

powder

Quality level:

100

Pricing and availability is not currently available.

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Properties

Quality Level

100

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

-10 to -25°C

SMILES string

NC(S1)=C(C#N)C2=C1CCC[C@]2(C)C3=NC(C4=NC(O[C@@H](C)[C@]5([H])CCCN5C)=CC=N4)=NO3

Description

Application

BI-2865 may be used for studying the Kirsten rat sarcoma virus (KRAS)signaling pathways and their role in cancer. Its selective inhibition of KRAS isused to probe the biological functions of KRAS, its mutants, and downstreamsignaling pathways to gain a deeper understanding of KRAS-related oncogenesis. [1][2]

Biochem/physiol Actions

BI-2865 is a cell penetrant, selective and potent pan-KRAS inhibitor, which binds with high affinity to the inactive state of KRAS and KRAS mutants. BI-2865 blocks nucleotide exchange to prevent the activation of wild-type KRAS and a broad range of KRAS mutants. It inhibits downstream signaling and growth in cancer cells harboring mutant KRAS. It does not bind to NRAS and HRAS.

pictograms

GHS07

signalword

Warning

hcodes

H302,H315

pcodes

P264 - P280 - P301 + P312 - P302 + P352 - P332 + P313 - P362 + P364

Hazard Classifications

Acute Tox. 4 Oral - Skin Irrit. 2

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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Pan-KRAS Inhibitors BI-2493 and BI-2865 Display Potent Antitumor Activity in Tumors with KRAS Wild-type Allele Amplification.

Antonio Tedeschi et al.

Molecular cancer therapeutics, 24(4), 550-562 (2024-12-23)

KRASG12C selective inhibitors, such as sotorasib and adagrasib, have raised hopes of targeting other KRAS-mutant alleles in patients with cancer. We report that KRAS wild-type (WT)-amplified tumor models are sensitive to treatment with the small-molecule KRAS inhibitors BI-2493 and BI-2865.

Pan-KRAS inhibitor disables oncogenic signalling and tumour growth.

Dongsung Kim et al.

Nature, 619(7968), 160-166 (2023-06-01)

KRAS is one of the most commonly mutated proteins in cancer, and efforts to directly inhibit its function have been continuing for decades. The most successful of these has been the development of covalent allele-specific inhibitors that trap KRAS G12C

A non-covalent inhibitor with pan-KRAS potential.

Katie Kingwell

Nature reviews. Drug discovery, 22(8), 622-622 (2023-07-07)

Global Trade Item Number

SKU	GTIN
SML4151-25MG	04065272613774
SML4151-5MG	04065272613781