AG-120 (Synonyms: Invosidenib) |
| カタログ番号GC15601 |
AG-120 (AG-120) は、イソクエン酸デヒドロゲナーゼ 1 変異体 (mIDH1) 酵素の経口活性阻害剤であり、in vivo で d-2-ヒドロキシグルタレート (2-HG) を大幅に低下させます。
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Cas No.: 1448347-49-6
Sample solution is provided at 25 µL, 10mM.
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IC50: < 100 nM
AG-120 is an IDH1 inhibitor.
Isocitrate dehydrogenase (IDH) is a metabolic enzyme interconverting isocitrate and α-ketoglutarate (α-KG), but cancer-associated mutations of IDH1 and IDH2 confer a neomorphic activity, which allows reduction of α-KG to the oncometabolite 2-HG.
In vitro: TF-1 cells or primary human AML patient samples expressing mutant IDH1 were treated with AG-120, and the results showed that in TF-1 IDH1-R132H cells, AG-120 was able to decrease the intracellular 2-HG levels, inhibit growth factor independent proliferation and restore erythropoietin-induced differentiation [1].
Ex vivo: Previous ex-vivo study showed that the pharmacological inhibition of mutant IDH1 enzyme with AG-120 in primary human blast cells led to an effective way to lower intracellular 2-HG levels and induced myeloid differentiation [1].
Clinical trial: In a phase I clinical trial, 62 patients with advanced IDH1 mutation–positive solid tumors were treated with single agent AG-120 orally once a day. Results showed that 7 of 11 patients with IDH1 mutant–positive chondrosarcoma had stable disease; 1 out of 20 patients with IDH1 mutant–positive IHCC had a partial response and 11 patients had SD; and one out of four patients with other IDH1 mutant–positive solid tumors had SD [2].
References:
[1] Erica Hansen et al. AG-120, an Oral, Selective, First-in-Class, Potent Inhibitor of Mutant IDH1, Reduces Intracellular 2HG and Induces Cellular Differentiation in TF-1 R132H Cells and Primary Human IDH1 Mutant AML Patient Samples Treated Ex Vivo. Blood 2014 124:3734.
[2] http://www. aacr.org/Newsroom/Pages/News-Release-Detail.aspx ItemID=789#.WLAUOm997IU
| Cas No. | 1448347-49-6 | SDF | |
| 同義語 | Invosidenib | ||
| Chemical Name | (S)-N-((S)-1-(2-chlorophenyl)-2-((3,3-difluorocyclobutyl)amino)-2-oxoethyl)-1-(4-cyanopyridin-2-yl)-N-(5-fluoropyridin-3-yl)-5-oxopyrrolidine-2-carboxamide | ||
| Canonical SMILES | O=C([C@H](CC1)N(C2=NC=CC(C#N)=C2)C1=O)N([C@@H](C3=CC=CC=C3Cl)C(NC4CC(F)(F)C4)=O)C5=CC(F)=CN=C5 | ||
| Formula | C28H22ClF3N6O3 | M.Wt | 582.96 |
| 溶解度 | ≥ 58.3mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.7154 mL | 8.5769 mL | 17.1538 mL |
| 5 mM | 0.3431 mL | 1.7154 mL | 3.4308 mL |
| 10 mM | 0.1715 mL | 0.8577 mL | 1.7154 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 3 reference(s) in Google Scholar.)
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