SAR405 - Moligand™, 10mM in DMSO , Inhibitor of phosphatidylinositol 3-kinase catalytic subunit type 3, CAS No.1523406-39-4, Inhibitor of phosphatidylinositol 3-kinase catalytic subunit type 3

CAS: 1523406-39-4 Cat. No.: S408270 分子式: C₁₉H₂₁ClF₃N₅O₂ 分子量: 443.85

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

4H-​Pyrimido[1,​2-​a]​pyrimidin-​4-​one, 9-​[(5-​chloro-​3-​pyridinyl)​methyl]​-​6,​7,​8,​9-​tetrahydro-​2-​[(3R)​-​3-​methyl-​4-​morpholinyl]​-​8-​(trifluoromethyl)​-​, (8S)​-

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

概要

Information

SAR405 SAR405 is a low-molecular-mass kinase inhibitor of PIK3C3/Vps34 (KD 1.5 nM) showing high selectivity and not be active up to 10 μM on class I and class II PI3Ks as well as on mTOR. SAR405 prevents autophagy and synergizes with MTOR (mechanistic t
In vitro

SAR405 is an inhibitor that was highly specific for Vps34 with regard to protein kinases and other phosphoinositide kinases. SAR405 has an IC50 of 1 nM in the phosphorylation of a PtdIns substrate by human recombinant Vps34 enzyme. This compound shows a binding equilibrium constant KD of 1.52 ± 0.77 nM (± s.d.) and a dissociation rate constant, k_off, of 3.03 ± 0.55 10⁻³/s, corresponding to a residence half-life, t_1/2, of 3.8 min. SAR405 does not affect the Akt phosphorylation at concentrations up to 10 μM in the PC3 cell line. SAR405 affects vesicle trafficking from late endosomes to lysosomes. It is also a potent autophagy inhibitor.

In vivo

Cell Data

cell lines：Ba/F3 cells expressing Bcr-Abl or a range of single mutations in the kinase domain of Bcr-Abl

Concentrations：1 μM

Incubation Time：4 h

Powder Purity:≥99%

Specifications

同義語

4H-​Pyrimido[1,​2-​a]​pyrimidin-​4-​one, 9-​[(5-​chloro-​3-​pyridinyl)​methyl]​-​6,​7,​8,​9-​tetrahydro-​2-​[(3R)​-​3-​methyl-​4-​morpholinyl]​-​8-​(trifluoromethyl)​-​, (8S)​-

仕様と純度

Moligand™, 10mM in DMSO

生化学的・生理学的メカニズム

SAR405 is a low-molecular-mass kinase inhibitor of PIK3C3/Vps34 (KD 1.5 nM) showing high selectivity and not be active up to 10 μM on class I and class II PI3Ks as well as on mTOR. SAR405 prevents autophagy and synergizes with MTOR (mechanistic target of

保管条件

Store at -80°C

入荷

Dry ice packs + Cold packs

この製品は冷冷この冷このこの製品の運送が必要です。地上およびその他の経済サービスは利用できません。

等級

Moligand™

アクションタイプ

INHIBITOR

作用メカニズム

Inhibitor of phosphatidylinositol 3-kinase catalytic subunit type 3

名前と識別子

• 異性体SMILES: C[C@@H]1COCCN1C2=CC(=O)N3CC[C@H](N(C3=N2)CC4=CC(=CN=C4)Cl)C(F)(F)F
• 分子量: 443.85

関連ターゲット（人間）

PIK3C3 Tchem Phosphatidylinositol 3-kinase catalytic subunit type 3 (5 Activities)

Discover Target: PIK3C3

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)