A-385358 - Moligand™,10mM in DMSO , CAS No.406228-55-5

CAS: 406228-55-5 Cat. No.: A656333 Formule: C₃₂H₄₁N₅O₅S₂ Poids moléculaire: 639.83 PubChem CID: 11556440

QUALITÉ & PURETÉ Moligand™, 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Vue d’ensemble

A-385358 is a selective inhibitor of Bcl-X L with K i s of 0.80 and 67 nM for Bcl-X L and Bcl-2 , respectively.

In Vitro

A-385358 is a selective inhibitor of Bcl-X L with K i s of 0.80 and 67 nM for Bcl-X L and Bcl-2, respectively, in fluorescence polarization assays. Treatment of IL-3-deprived FL5.12/Bcl-X L cells for 24 hours with A-385358 results in cell killing with an EC 50 of 0.47±0.05 μM (n=68). This effect is accompanied by an increase in caspase-3 activity. Consistent with the greater affinity for the Bcl-X L versus Bcl-2 hydrophobic grooves, the EC 50 of A-385358 for IL-3-depleted FL5.12/Bcl-2 cells (1.9±0.1 μM; n=55) is 4-fold higher relative to the cytokine-deprived FL5.12/Bcl-X L cells. In addition, A-385358 is more effective at stimulating cytochrome c release from mitochondria isolated from FL5.12/Bcl-X L versus Bcl-2 cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

The combination of A-385358 given at 100 mg/kg/d plus the lower dose of paclitaxel produces a significant reduction in tumor growth (%T/C) compare with paclitaxel monotherapy. This combination also yields a >100% increase in time for tumors to reach 900 mm 3 (%ILS) compare with vehicle control. Maximal efficacy is observed during the dosing period for A-385358, with slow but steady increase in the tumor growth after termination of treatment. The combination of A-385358 at 75 mg/kg/d plus paclitaxel at 30 mg/kg/d is also well tolerated and inhibits tumor growth rate by nearly 80%. Significant effects on tumor growth relative to paclitaxel monotherapy are observed with doses as low as 50 mg/kg/d . MCE has not independently confirmed the accuracy of these methods. They are for reference only.

IC50& Target:Bcl-xL 0.8 nM (Ki) Bcl-2 67 nM (Ki)

Spécifications

Spécifications et pureté

Moligand™,10mM in DMSO

Mécanismes biochimiques et physiologiques

A-385358 is a selective inhibitor of Bcl-X L with K i s of 0.80 and 67 nM for Bcl-X L and Bcl-2 , respectively.

Conditions de stockage de stockage

Store at -80°C

Expédié en

Dry ice packs + Cold packs

Ce produit nécessite l'expédition en chaîne froide. Les services terrestres et autres services économiques ne sont pas disponibles.

Grade

Moligand™

Type d'action

INHIBITOR

Noms et identifiants

Isomères SMILES

CC1(CCN(CC1)C2=CC=C(C=C2)C(=O)NS(=O)(=O)C3=CC(=C(C=C3)N[C@H](CCN(C)C)CSC4=CC=CC=C4)[N+](=O)[O-])C

PubChem CID

11556440

Poids moléculaire

639.83

Cibles associées (humaines)

BCL2 Tclin Apoptosis regulator Bcl-2 (3 Activities)

Discover Target: BCL2

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

BCL2L1 Tchem Bcl-2-like protein 1 (19 Activities)

Discover Target: BCL2L1

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

BCL2L2 Tchem Bcl-2-like protein 2 (1 Activities)

Discover Target: BCL2L2

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

Foire aux questions

What is Moligand??

Moligand? is one of Aladdin Scientific's premium product lines, formulated for high-purity applications across multiple workflows. Compared to standard grades in the same workflow, Moligand? products typically offer tighter specifications, more rigorous QC, and stronger lot-to-lot consistency.

How should this product be stored?

Store at ?80 °C. Ultra-low temperature storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships frozen with dry ice and cold packs. Unpack on arrival and transfer it to the storage condition stated above; handle dry ice with insulated gloves in a ventilated area.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 406228-55-5, the molecular formula is C32H41N5O5S2, and the molecular weight is 639.83 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.