AMG 511


Catalog No. Size PriceQuantity
M23819-C Contact sales@xcessbio.com for quotation $100Unavailable

Description

AMG 511 is a potent and orally available pan inhibitor of class I PI3Ks, with Kis 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.

Product information

CAS Number: 1253573-53-3

Molecular Weight: 517.58

Formula: C22H28FN9O3S

Chemical Name: 4-{2-[(5-fluoro-6-methoxypyridin-3-yl)amino]-5-[(1R)-1-(4-methanesulfonylpiperazin-1-yl)ethyl]pyridin-3-yl}-6-methyl-1,3,5-triazin-2-amine

Smiles: CC1N=C(N=C(N)N=1)C1=CC(=CN=C1NC1=CC(F)=C(N=C1)OC)[C@@H](C)N1CCN(CC1)S(C)(=O)=O

InChiKey: KUGIFHQBIIHRIZ-CYBMUJFWSA-N

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

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 33.33 mg/mL (64.40 mM; Need ultrasonic).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

AMG 511 shows the inhibition of AKT (Ser473) phosphorylation in U87 malignant glioma (MG) cells with an IC50 of 4 nM.

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.

Products are for research use only. Not for human use.

Payment & Security

PayPal Venmo

Your payment information is processed securely. We do not store credit card details nor have access to your credit card information.

You may also like

Recently viewed