Product Name :
AMG319
Description:
AMG319 is a potent and selective PI3Kδ kinase inhibitor with IC50 of 18 nM.
CAS:
1608125-21-8
Molecular Weight:
385.40
Formula:
C21H16FN7
Chemical Name:
N-[(1S)-1-[7-fluoro-2-(pyridin-2-yl)quinolin-3-yl]ethyl]-9H-purin-6-amine
Smiles :
C[C@H](NC1=NC=NC2NC=NC=21)C1=CC2=CC=C(F)C=C2N=C1C1=CC=CC=N1
InChiKey:
KWRYMZHCQIOOEB-LBPRGKRZSA-N
InChi :
InChI=1S/C21H16FN7/c1-12(28-21-19-20(25-10-24-19)26-11-27-21)15-8-13-5-6-14(22)9-17(13)29-18(15)16-4-2-3-7-23-16/h2-12H,1H3,(H2,24,25,26,27,28)/t12-/m0/s1
Purity:
≥98% (or refer to the Certificate of Analysis)
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.
Additional information:
AMG319 is a potent and selective PI3Kδ kinase inhibitor with IC50 of 18 nM.|Product information|CAS Number: 1608125-21-8|Molecular Weight: 385.40|Formula: C21H16FN7|Chemical Name: N-[(1S)-1-[7-fluoro-2-(pyridin-2-yl)quinolin-3-yl]ethyl]-9H-purin-6-amine|Smiles: C[C@H](NC1=NC=NC2NC=NC=21)C1=CC2=CC=C(F)C=C2N=C1C1=CC=CC=N1|InChiKey: KWRYMZHCQIOOEB-LBPRGKRZSA-N|InChi: InChI=1S/C21H16FN7/c1-12(28-21-19-20(25-10-24-19)26-11-27-21)15-8-13-5-6-14(22)9-17(13)29-18(15)16-4-2-3-7-23-16/h2-12H,1H3,(H2,24,25,26,27,28)/t12-/m0/s1|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: DMSO : 50 mg/mL (129.74 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:|AMG319 inhibits PI3Kδ, PI3Kγ, PI3Kβ and PI3Kα with IC50s of 18 nM, 850 nM, 2.7 μM and 33 μM, respectively. AMG319, a compound with an IC50 of 16 nM in a human whole blood assay (HWB), excellent selectivity over a large panel of protein kinases, and a high level of in vivo efficacy as measured by two rodent disease models of inflammation.Siponimod web AMG319 has minimal CYP3A4/2D6 inhibition and does not inhibit CYPs (1A2, 2C8, 2C9, 2C19, 2E1, all >20 μM).Cediranib VEGFR There is no time dependent inhibition (TDI) against CYPs 3A4, 2D6, 1A2, and 2C9 nor CYP induction (3A4, 2D6, 1A2, 2B6) as measured in hepatocytes.PMID:31644056 AMG319 is clean in a hERG binding assay (>25 μM), and an Ames micronucleus test proved negative. AMG319 has minimal effects in a BSEP assay up to >200 μM. Additionally, AMG319 is clean in a large side effect profiling panel (CEREP) and has no activity in a large panel of 359 unique protein kinases tested at 10 μM drug concentration.|In Vivo:|The study is performed to determine the correlation between biochemical coverage (i.e., pAKT) with functional activity in vivo. AMG319 achieves this coverage at the 3 mg/kg level, which also coveres the human whole blood assay (HWB) (CD-69) IC90 at trough for a full 24 h period. The lower doses 0.1, 0.3, and 1 mg/kg cover trough concentrations between the HWB IC50 and IC90 and evince partial efficacy. Similarly, the plasma concentration of AMG319 covers the IC90 at the 1 mg/kg dose of the mouse anti-IgM pAKT in vitro assay.|Products are for research use only. Not for human use.|
