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AMG 511 - 99%, high purity , CAS No.1253573-53-3

COA COA
    Grade & Purity:
  • ≥99%
In stock
Item Number
A651027
Grouped product items
SKU Size
Availability
 Price Qty
A651027-1mg
1mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$104.90
A651027-5mg
5mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$220.90
A651027-10mg
10mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$420.90
A651027-25mg
25mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$940.90
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PI3K (243) PI3K/Akt/mTOR (765)

Basic Description

Specifications & Purity ≥99%
Biochemical and Physiological Mechanisms AMG 511 is a potent and orally available pan inhibitor of class I PI3K s, with K i s of 4 nM, 6 nM, 2 nM and 1 nM for PI3Kα , β, δ and γ, respectively. AMG 511 significantly suppresses PI3K signaling that is indicated by p-Akt (Ser473) decrease. AMG 511 e
Storage Temp Store at -20°C
Shipped In
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This product requires cold chain shipping. Ground and other economy services are not available.
Product Description

AMG 511 is a potent and orally available pan inhibitor of class I PI3K s, with K i s of 4 nM, 6 nM, 2 nM and 1 nM for PI3Kα , β, δ and γ, respectively. AMG 511 significantly suppresses PI3K signaling that is indicated by p-Akt (Ser473) decrease. AMG 511 exhibits anti-tumor activity in mouse glioblastoma xenograft model

In Vitro

AMG 511 shows the inhibition of AKT (Ser473) phosphorylation in U87 malignant glioma (MG) cells with an IC 50 of 4 nM. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

AMG 511 potently blocks 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) . AMG 511 shows excellent in vivo efficacy and pharmacokinetic profile . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Female CD1 NU/NU mice, with U87 MG glioblastoma xenograft model Dosage: 1 mg/kg, 3 mg/kg, 10 mg/kg Administration: Oral administration, daily, for 12 days Result: Inhibited tumor growth. Animal Model: Male Sprague-Dawley rats Dosage: 1 mg/kg Administration: Oral administration (Pharmacokinetic Analysis) Result: Had a superior pharmacokinetic profile with low clearance (0.4 L/h/kg, 12% of liver blood flow), good oral bioavailability (F = 60%), and a commensurate high oral exposure (AUC = 5.0 μM·h).

Form:Solid

IC50& Target:PI3Kα 4 nM (Ki) PI3Kβ 6 nM (Ki) PI3Kδ 2 nM (Ki) PI3Kγ 1 nM (Ki)

Taxonomic Classification

Taxonomy Tree

Kingdom Organic compounds
Superclass Organoheterocyclic compounds
Class Triazines
Subclass Aminotriazines
Intermediate Tree Nodes Not available
Direct Parent Aminotriazines
Alternative Parents Alkyl aryl ethers  Aminopyridines and derivatives  Aralkylamines  N-alkylpiperazines  1,3,5-triazines  Aryl fluorides  Imidolactams  Organic sulfonamides  Organosulfonamides  Sulfonyls  Heteroaromatic compounds  Trialkylamines  Azacyclic compounds  Secondary amines  Hydrocarbon derivatives  Primary amines  Organic oxides  Organofluorides  
Molecular Framework Aromatic heteromonocyclic compounds
Substituents Alkyl aryl ether - Aminopyridine - Amino-1,3,5-triazine - Aminotriazine - N-alkylpiperazine - Aralkylamine - Piperazine - 1,4-diazinane - Pyridine - Aryl halide - Organic sulfonic acid amide - Organosulfonic acid amide - 1,3,5-triazine - Aryl fluoride - Imidolactam - Heteroaromatic compound - Organosulfonic acid or derivatives - Organic sulfonic acid or derivatives - Sulfonyl - Tertiary amine - Tertiary aliphatic amine - Azacycle - Secondary amine - Ether - Organofluoride - Organohalogen compound - Organic oxygen compound - Primary amine - Amine - Organic nitrogen compound - Hydrocarbon derivative - Organic oxide - Organonitrogen compound - Organooxygen compound - Organosulfur compound - Aromatic heteromonocyclic compound
Description This compound belongs to the class of organic compounds known as aminotriazines. These are organic compounds containing an amino group attached to a triazine ring.
External Descriptors Not available

Associated Targets(Human)

PIK3CG Tclin Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
PIK3CA Tclin Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
MTOR Tclin Serine/threonine-protein kinase mTOR (13850 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PIK3CG Tclin PI3-kinase p110-gamma subunit (5411 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Liver microsomes (16955 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PIK3C3 Tchem Phosphatidylinositol 3-kinase catalytic subunit type 3 (535 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PIK3R1 Tchem PI3-kinase p110-delta/p85-alpha (1508 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PIK3R1 Tchem PI3-kinase p110-alpha/p85-alpha (2589 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

Associated Targets(non-human)

PIK3CA PI3-kinase p110-alpha subunit (51 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Mus musculus (284745 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Rattus norvegicus (775804 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
LLC-PK1 (2135 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Plasma (328 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Liver microsome (341 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

Mechanisms of Action

Mechanism of Action Action Type target ID Target Name Target Type Target Organism Binding Site Name References

Names and Identifiers

IUPAC Name 4-[2-[(5-fluoro-6-methoxypyridin-3-yl)amino]-5-[(1R)-1-(4-methylsulfonylpiperazin-1-yl)ethyl]pyridin-3-yl]-6-methyl-1,3,5-triazin-2-amine
INCHI 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
InChIKey KUGIFHQBIIHRIZ-CYBMUJFWSA-N
Smiles CC1=NC(=NC(=N1)N)C2=C(N=CC(=C2)C(C)N3CCN(CC3)S(=O)(=O)C)NC4=CC(=C(N=C4)OC)F
Isomeric SMILES CC1=NC(=NC(=N1)N)C2=C(N=CC(=C2)[C@@H](C)N3CCN(CC3)S(=O)(=O)C)NC4=CC(=C(N=C4)OC)F
PubChem CID 56947516
Molecular Weight 503.55

Certificates（CoA,COO,BSE/TSE and Analysis Chart)

C of A & Other Certificates(BSE/TSE, COO):
Analytical Chart:

Chemical and Physical Properties

Solubility DMSO : 33.33 mg/mL (64.40 mM; Need ultrasonic)
Molecular Weight 517.600 g/mol
XLogP3 1.100
Hydrogen Bond Donor Count 2
Hydrogen Bond Acceptor Count 13
Rotatable Bond Count 7
Exact Mass 517.202 Da
Monoisotopic Mass 517.202 Da
Topological Polar Surface Area 161.000 Ų
Heavy Atom Count 36
Formal Charge 0
Complexity 813.000
Isotope Atom Count 0
Defined Atom Stereocenter Count 1
Undefined Atom Stereocenter Count 0
Defined Bond Stereocenter Count 0
Undefined Bond Stereocenter Count 0
The total count of all stereochemical bonds 0
Covalently-Bonded Unit Count 1

Solution Calculators

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