About 8 results found for searched term "Mutant IDH1-IN-4" (0.173 seconds)
| Cat.No. | Name | Target |
|---|---|---|
| M54537 | Mutant IDH1-IN-4 | Isocitrate Dehydrogenase (IDH) |
| Mutant IDH1-IN-4 is an inhibitor of mutant isocitrate dehydrogenase 1 (IDH 1) with an IC50 value of ≤ 0.5 μM for mutant IDH 1 in R132H, HT1080 and U87R132H cells. | ||
| M10335 | IDH-305 | Isocitrate Dehydrogenase (IDH) |
| IDH305 | ||
| IDH-305 is an orally available, mutant-selective and brain-penetrant IDH1 inhibitor that targets IDH1(R132) mutation with IC50 values of 27 nM, 28 nM and 6.14 μM for IDH1R132H, IDH1R132C and IDH1WT, respectively. | ||
| M10434 | Olutasidenib (FT-2102) | Isocitrate Dehydrogenase (IDH) |
| FT-2102 | ||
| Olutasidenib (FT-2102) is a highly potent and selective, orally active, brain penetrant mutant Isocitrate dehydrogenase 1 (IDH1) inhibitor, with IC50 values of 21.2 nM and 114 nM for IDH1- R132H and IDH1- R132C, respectively. | ||
| M11277 | IDH889 | Isocitrate Dehydrogenase (IDH) |
| IDH889 is an orally available, brain permeable, allosteric and mutation-specific inhibitor of isocitrate dehydrogenase (IDH1). IDH889 showed high selectivity against IDH1R132 * mutant, with IC50 values of 0.02 μM, 0.072 μM and 1.38 μM against IDH1R132H, IDH1R132C and IDH1wt, respectively. IDH889 showed high inhibition of intracellular 2-Hg level with IC50 value of 0.014 μM. | ||
| M14454 | Mutant IDH1-IN-1 | Isocitrate Dehydrogenase (IDH) |
| Mutant IDH1-IN-1 is a mutant-selective IDH1 inhibitor with with IC50s of 4, 42, 80 and 143 nM against mutant IDH1 R132C/R132C, IDH1 R132H/R132H, IDH1 R132H/WT and wild type IDH1, respectively. | ||
| M54530 | (1R)-IDH889 | Isocitrate Dehydrogenase (IDH) |
| (1R)-IDH889 is the inactive isomer of IDH889, which serves as a control compound in experiments.IDH889 is an orally active, brain-permeable, variant- and mutation-specific inhibitor of isocitrate dehydrogenase (IDH1).IDH889 is highly selective for the IDH1 R132 mutant, and acts efficiently on IDH1R132H, IDH1R132C and IDH1wt with IC50 values of 0.02 μM, 0.072 μM and 1.38 μM, respectively.In addition, IDH889 has a potent and potent effect on IDH1R132C and IDH1wt, IDH889 is highly selective for the IDH1 R132 mutant, with IC50 values of 0.02 μM, 0.072 μM, and 1.38 μM for IDH1R132H, IDH1R132C, and IDH1wt, respectively, and has a high potency to inhibit the level of intracellular 2-HG, with an IC50 value of 0.014 μM. | ||
| M54531 | (S,R)-GSK321 | Isocitrate Dehydrogenase (IDH) |
| (S,R)-GSK321 is a potent and selective inhibitor of mutant IDH1, inhibiting R132G, R132C, R132H, and WT IDH1 with IC50 values of 2.9, 3.8, 4.6, and 46 nM, respectively, with a 100-fold higher selectivity than IDH2. (S,R)-GSK321 induces a reduction in intracellular 2-HG, failure of myeloid differentiation blockade, and induction of granulocyte differentiation at the level of leukemoblasts and more immature stem cells. (S,R)-GSK321 can be used in studies related to acute myeloid leukemia (AML) and other cancers. | ||
| M54535 | IDH1 Inhibitor 1 | Isocitrate Dehydrogenase (IDH) |
| IDH1 Inhibitor 1 is a potent, orally bioavailable, brain-permeable, selective mutant IDH1 inhibitor that inhibits IDH1R132H, IDH1R132C, and IDH1WT with IC50s of 0.021 μM, 0.045 μM, and 2.52 μM, respectively. possesses antitumor activity. | ||
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