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BI-2852

BI-2852

Item no.	HY-126247-25mg
Manufacturer	MedChem Express
CASRN	2375482-51-0
Amount	25 mg
Quantity options	100 mg 10 mM/1 mL 10 mg 25 mg 50 mg 5 mg
Category	Inhibitors & Compound Libraries Small Molecules
Type	Inhibitors
Specific against	other
Purity	99.57
Citations	[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
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
ECLASS 10.1	32160490
ECLASS 11.0	32160490
UNSPSC	12000000
Shipping Condition	Room temperature
Available
Manufacturer - Type	Reference compound
Manufacturer - Applications	Neuroscience-Neuromodulation
Manufacturer - Targets	Ras
Shipping Temperature	Room Temperature
Storage Conditions	4°C (Powder, stored under nitrogen)
Molecular Weight	516.59
Product Description	BI-2852 is a KRAS inhibitor for the switch I/II pocket (SI/II-pocket) by structure-based agent 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.
Manufacturer - Research Area	Cancer
Solubility	DMSO: 55 mg/mL (ultrasonic)
Manufacturer - Pathway	GPCR/G Protein; MAPK/ERK Pathway
Isoform	K-Ras
Clinical information	No Development Reported

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HY-126247-25mg-safety-datasheet.pdf