An inhibitor of the K-Ras-SOS1 protein-protein interaction

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BI-3406

Name: BI-3406
Brand: -

Item No. 35261

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)

Technical Information

Formal Name

N-[(1R)-1-[3-amino-5-(trifluoromethyl)phenyl]ethyl]-7-methoxy-2-methyl-6-[[(3S)-tetrahydro-3-furanyl]oxy]-4-quinazolinamine

CAS Number

2230836-55-0

Molecular Formula

C₂₃H₂₅F₃N₄O₃

Formula Weight

462.5

Purity

≥98%

Formulation (Request formulation change)

A solid

Solubility(Learn about Variance in Solubility)

DMF: 3 mg/mlDMSO: 2 mg/mlEthanol: 10 mg/mlPBS (pH 7.2): insol

λ_max

246 nm

SMILES

C[C@H](C1=CC(C(F)(F)F)=CC(N)=C1)NC2=NC(C)=NC3=C2C=C(O[C@H]4CCOC4)C(OC)=C3

InChi Code

InChI=1S/C23H25F3N4O3/c1-12(14-6-15(23(24,25)26)8-16(27)7-14)28-22-18-9-21(33-17-4-5-32-11-17)20(31-3)10-19(18)29-13(2)30-22/h6-10,12,17H,4-5,11,27H2,1-3H3,(H,28,29,30)/t12-,17+/m1/s1

InChi Key

XVFDNRYZXDHTHT-PXAZEXFGSA-N

Shipping & Storage Information

Storage

-20°C

Shipping

Room temperature in continental US; may vary elsewhere

Certificates of Analysis & Batch Specific Data

Provide batch numbers separated by commas to download or request available product inserts, QC sheets, certificates of analysis, data packs, and GC-MS data.

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1 mg

$69

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5 mg

$233

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10 mg

$427

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25 mg

$737

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Product Description

BI-3406 is an inhibitor of the protein-protein interaction between K-Ras and the guanine nucleotide exchange factor son of sevenless homolog 1 (SOS1; IC₅₀ = 5 nM).¹ It selectively disrupts the protein-protein interaction between K-Ras^G12C or K-Ras^G12D with SOS1 over SOS2, and it is selective over 321 kinases in a panel at 10 µM but does inhibit PLK4, BMPR2, and LRRK2 activity by greater than 50%. BI-3406 inhibits the growth of DLD-1, A549, NCI H23, and NCI H358 cells expressing mutant K-Ras (IC₅₀s = 16-52 nM) but not NCI H520 and A375 cells expressing wild-type K-Ras. BI-3406 (12 or 50 mg/kg, twice per day) reduces tumor growth in an MIA PaCa-2 mouse xenograft model.

WARNING This product is not for human or veterinary use.

References & Product Citations

Product Description References

1. Hofmann, M.H., Gmachl, M., Ramharter, J., et al. BI-3406, a potent and selective SOS1-KRAS interaction inhibitor, is effective in KRAS-driven cancers through combined MEK inhibition. Cancer Discov. 11(1), 142-157 (2021).

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