Product Data Sheet
(S,R)-GSK321
Catalog No. A75789
(S,R)-GSK321 is the (S,R)-enantiomer of GSK321, a selective inhibitor of mutant isocitrate dehydrogenase 1 (IDH1). It exhibits potent inhibitory activity with IC50 values of 2.9 nM for R132G, 3.8 nM for R132C, 4.6 nM for R132H, and 46 nM for wild-type IDH1, displaying over 100-fold selectivity for IDH1 compared to IDH2. This compound effectively reduces intracellular levels of 2-hydroxyglutarate (2-HG), alleviates the myeloid differentiation block, and promotes granulocytic differentiation in leukemic blasts and stem-like cells. (S,R)-GSK321 is relevant for research into acute myeloid leukemia (AML) and related malignancies.
Chemical Information
| Catalog Num | A75789 |
|---|---|
| M. Wt | 501.55 |
| Formula | C28H28FN5O3 |
| Purity | >98% |
| Storage | at -20 °C 3 years (powder form); at -20 °C 6 months (Solution base) |
| CAS No. | 1816272-18-0 |
| Synonyms | |
| SMILES | C[C@@H](O)C1=CC=CC(NC(C2=NN(C3=C2CN(C[C@@H]3C)C(C4=CC=CN4)=O)CC5=CC=C(C=C5)F)=O)=C1 |
Biological Activity
| Description | (S,R)-GSK321 is the (S,R)-enantiomer of GSK321, a selective inhibitor of mutant isocitrate dehydrogenase 1 (IDH1). It exhibits potent inhibitory activity with IC50 values of 2.9 nM for R132G, 3.8 nM for R132C, 4.6 nM for R132H, and 46 nM for wild-type IDH1, displaying over 100-fold selectivity for IDH1 compared to IDH2. This compound effectively reduces intracellular levels of 2-hydroxyglutarate (2-HG), alleviates the myeloid differentiation block, and promotes granulocytic differentiation in leukemic blasts and stem-like cells. (S,R)-GSK321 is relevant for research into acute myeloid leukemia (AML) and related malignancies. |
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RETURN POLICY
Adooq’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.
Adooq’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
Adooq products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Adooq 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 Adooq products are stable under the recommended conditions.
Adooq products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Adooq 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 Adooq products are stable under the recommended conditions.
