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Formula | C23H25F3N4O3 |
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Molecular Weight | 462.46 | CAS No. | 2230836-55-0 | |
Solubility (25°C)* | In vitro | DMSO | 92 mg/mL (198.93 mM) | |
Ethanol | 92 mg/mL (198.93 mM) | |||
Water | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
Description | BI-3406 (compound I-13) is a potent, selective and orally active inhibitor of the interaction between KRAS and Son of Sevenless 1 (SOS1) with IC50 of 5 nM. BI-3406 reduces the formation of GTP-loaded KRAS, and inhibits MAPK pathway signaling. BI-3406 exhibits anti-tumor activities. | ||
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Targets |
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In vitro | BI-3406, a selective SOS1 inhibitor, enhanced the AMG 510-induced growth suppression in MIA PaCa-2 cells. Treatment with 5 µM BI-3406 following the excision of endogenous mutant KRAS abolishes both ERK and AKT activation, consistent with the inhibition of WT RAS signaling.[1] |
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In vivo | BI-3406, a potent and selective SOS1-KRAS Interaction Inhibitor, is effective in KRAS-driven cancers through combined MEK inhibition.[2] |
Description | BI-3406 (compound I-13) is a potent, selective and orally active inhibitor of the interaction between KRAS and Son of Sevenless 1 (SOS1) with IC50 of 5 nM. BI-3406 reduces the formation of GTP-loaded KRAS, and inhibits MAPK pathway signaling. BI-3406 exhibits anti-tumor activities. | ||
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Targets |
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KRASG 12C-inhibitor-based combination therapies for pancreatic cancer: insights from drug screening [ Mol Oncol, 2024, 10.1002/1878-0261.13725] | PubMed: 39253995 |
RAS-dependent RAF-MAPK hyperactivation by pathogenic RIT1 is a therapeutic target in Noonan syndrome-associated cardiac hypertrophy [ Sci Adv, 2023, 9(28):eadf4766] | PubMed: 37450595 |
RAS-dependent RAF-MAPK hyperactivation by pathogenic RIT1 is a therapeutic target in Noonan syndrome-associated cardiac hypertrophy [ Sci Adv, 2023, 9(28):eadf4766] | PubMed: 37450595 |
Impaired proteolysis of non-canonical RAS proteins drives clonal hematopoietic transformation [ Cancer Discov, 2022, CD-21-1631] | PubMed: 35904492 |
In vivo genome-wide CRISPR screening identifies ZNF24 as a negative NF-κB modulator in lung cancer [ Cell Biosci, 2022, 12(1):193] | PubMed: 36457047 |
Profiling oncogenic KRAS mutant drugs with a cell-based Lumit p-ERK immunoassay [ SLAS Discov, 2022, S2472-5552(22)12517-7] | PubMed: 35288294 |
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.