| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 100mg |
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Purity: ≥98%
AMG-511 is a potent and selective pan class I PI3K inhibitor exhibiting IC50 of 8, 11, 2, and 6 nM against the PI3K β, α, β, and ≤ isoforms respectively. AMG 511 reduced AKT S473 phosphorylation in a dose-dependent manner in U87 MG glioblastoma cells (IC50 = 4 nM), indicating that it inhibited PI3K pathway signaling. A downstream effector of AKT, PRAS40, was less phosphorylated as a result of AKT inhibition (IC50 = 23 nM). Additionally, U87 MG cells showed decreased phosphorylation of the mTORC1 substrates p70S6K (IC50 = 30 nM) and S6 (IC50 = 70 nM), but not 4EBP1 (T37/46).
| Targets |
PI3Kα (Ki = 4 nM); PI3Kβ (Ki = 6 nM); PI3Kδ (Ki = 2 nM); PI3Kγ (Ki = 1 nM)
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|---|---|
| ln Vitro |
AMG 511 shows the inhibition of AKT (Ser473) phosphorylation in U87 malignant glioma (MG) cells with an IC50 of 4 nM[1].
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| ln Vivo |
AMG 511 potently inhibits the targeted PI3K pathway in a mouse liver pharmacodynamic model (3-30 mg/kg; p.o.) and inhibits tumor growth in a U87 MG glioblastoma xenograft model (3-30 mg/kg; p.o.; daily; for 12 days)[1].
AMG 511 shows excellent in vivo efficacy and pharmacokinetic profile[1].
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| References |
| Molecular Formula |
C22H28FN9O3S
|
|---|---|
| Molecular Weight |
517.5796251297
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| Exact Mass |
517.202
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| Elemental Analysis |
C, 51.05; H, 5.45; F, 3.67; N, 24.36; O, 9.27; S, 6.19
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| CAS # |
1253573-53-3
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| Related CAS # |
1253573-53-3
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| PubChem CID |
56947516
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
3.359
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
13
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
36
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| Complexity |
813
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| Defined Atom Stereocenter Count |
1
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| SMILES |
S(C)(N1CCN([C@H](C)C2C=NC(=C(C3N=C(N)N=C(C)N=3)C=2)NC2C=NC(=C(C=2)F)OC)CC1)(=O)=O
|
| InChi Key |
KUGIFHQBIIHRIZ-CYBMUJFWSA-N
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| InChi Code |
InChI=1S/C22H28FN9O3S/c1-13(31-5-7-32(8-6-31)36(4,33)34)15-9-17(20-27-14(2)28-22(24)30-20)19(25-11-15)29-16-10-18(23)21(35-3)26-12-16/h9-13H,5-8H2,1-4H3,(H,25,29)(H2,24,27,28,30)/t13-/m1/s1
|
| Chemical Name |
(R)-4-[2-[(5-fluoro-6-methoxypyridin-3-yl)amino]-5-[1-(4-methylsulfonylpiperazin-1-yl)ethyl]pyridin-3-yl]-6-methyl-1,3,5-triazin-2-amine
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| Synonyms |
AMG511; AMG 511; AMG-511
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~33.3 mg/mL (~64.4 mM)
Water: ~8 mg/mL (~17.3 mM) Ethanol: <1 mg/mL |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2 mg/mL (3.86 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9321 mL | 9.6603 mL | 19.3207 mL | |
| 5 mM | 0.3864 mL | 1.9321 mL | 3.8641 mL | |
| 10 mM | 0.1932 mL | 0.9660 mL | 1.9321 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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