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Technical Data
| Formula | C32H47FN6O4S |
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| Molecular Weight | 630.82 | CAS No. | 2169916-18-9 | |
| Solubility (25°C)* | In vitro | DMSO | 100 mg/mL (158.52 mM) | |
| Ethanol | 100 mg/mL (158.52 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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Biological Activity
| Description | VTP50469 is a potent, highly selective and orally active inhibitor of Menin-MLL interaction with Ki of 104 pM. VTP50469 exhibits anti-leukemia activity. | ||
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| In vitro | Cell lines carrying MLL-rearrangements are selectively responsive to VTP50469. VTP50469 displaces Menin from protein complexes and inhibits chromatin occupancy of MLL at select genes. Loss of MLL binding leads to changes in gene expression, differentiation, and apoptosis.[2] |
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| In vivo | Patient-derived xenograft (PDX) models derived from patients with either MLL-r AML or MLL-r ALL shows dramatic reductions of leukemia burden when treated with VTP50469. Multiple mice engrafted with MLL-r ALL remains disease free greater than one year after treatment.[2] |
Biological Activity
| Description | VTP50469 is a potent, highly selective and orally active inhibitor of Menin-MLL interaction with Ki of 104 pM. VTP50469 exhibits anti-leukemia activity. | ||
|---|---|---|---|
| Targets |
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Protocol (from reference)
Selleck's VTP50469 has been cited by 4 publications
| Arachidonic acid released by PIK3CA mutant tumor cells triggers malignant transformation of colonic epithelium by inducing chromatin remodeling [ Cell Rep Med, 2024, S2666-3791(24)00179-4] | PubMed: 38614093 |
| MLL1 regulates cytokine-driven cell migration and metastasis [ Sci Adv, 2024, 10(11):eadk0785] | PubMed: 38478601 |
| Chemical-induced epigenome resetting for regeneration program activation in human cells [ Cell Rep, 2023, 42(6):112547] | PubMed: 37224020 |
| CRISPR-ChIP delineates a Menin-dependent oncogenic DOT1L complex in MLL-leukaemia [ bioRxiv, 2023, 10.1101/2023.03.17.533231] | PubMed: None |
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.