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Technical Data
| Formula | C26H22FN7O3 |
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| Molecular Weight | 499.5 | CAS No. | 1202759-32-7 | |
| Solubility (25°C)* | In vitro | DMSO | 100 mg/mL (200.2 mM) | |
| Ethanol | 2 mg/mL (4.0 mM) | |||
| Water | Insoluble | |||
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* <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.) |
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Preparing Stock Solutions
Biological Activity
| Description | CNX-774 is an irreversible, orally active, and highly selective BTK inhibitor with IC50 of <1 nM. | ||
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| Targets |
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| In vitro | In cellular assays, CNX-774 demonstrates potent inhibitory activity towards BTK with IC50 of 1-10 nM by targeting Cys-481 residue within the ATP binding site of the enzyme. [1] | ||
| Features | Orally bioavailable BTK-selective inhibitor, binding covalently to target protein. |
Protocol (from reference)
Customer Product Validation
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, , Allergy, 2017, 72(11):1666-1676
Selleck's CNX-774 has been cited by 5 publications
| ENT1 blockade by CNX-774 overcomes resistance to DHODH inhibition in pancreatic cancer [ Cancer Lett, 2023, 552:215981] | PubMed: 36341997 |
| Bruton's TK regulates myeloid cell recruitment during acute inflammation [ Br J Pharmacol, 2022, 179(11):2754-2770] | PubMed: 34897650 |
| Bruton's agammaglobulinemia tyrosine kinase (Btk) regulates TPA‑induced breast cancer cell invasion via PLCγ2/PKCβ/NF‑κB/AP‑1‑dependent matrix metalloproteinase‑9 activation [ Oncol Rep, 2021, 45(5)56] | PubMed: 33760219 |
| BTK inhibition is a potent approach to block IgE-mediated histamine release in human basophils. [Smiljkovic D, et al. Allergy, 2017, 10.1111/all.13166] | PubMed: 28328081 |
| The molecular mechanisms involved in lectin-induced human platelet aggregation. [ Biol Chem, 2017, 398(12):1335-1346] | PubMed: 28779561 |
RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
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.