Description
AQX-435 is a potent SHIP1 phosphatase activator. AQX-435 reduces PI3K activation downstream of the B-cell receptor (BCR) and induces apoptosis of malignant B cells, and reduces lymphoma growth.
Product information
CAS Number: 1619983-52-6
Molecular Weight: 450.57
Formula: C27H34N2O4
Chemical Name: N-[(2R,3S,4S,4aS,8aS)-4-(3,5-dihydroxybenzoyl)-3,4a,8,8-tetramethyl-decahydronaphthalen-2-yl]pyridine-3-carboxamide
Smiles: CC1(C)CCC[C@@]2(C)[C@H]1C[C@@H](NC(=O)C1=CN=CC=C1)[C@@H](C)[C@@H]2C(=O)C1C=C(O)C=C(O)C=1
InChiKey: JBBCDNNDYGLMOE-LZITZJIASA-N
InChi: InChI=1S/C27H34N2O4/c1-16-21(29-25(33)17-7-5-10-28-15-17)14-22-26(2,3)8-6-9-27(22,4)23(16)24(32)18-11-19(30)13-20(31)12-18/h5,7,10-13,15-16,21-23,30-31H,6,8-9,14H2,1-4H3,(H,29,33)/t16-,21-,22+,23-,27+/m1/s1
Technical Data
Appearance: Solid Power
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.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
AQX-435 reduces CLL cell viability in a dose-dependent manner. AQX-435-induced (5-30 µM; 24 hours) apoptosis is mediated via caspases since AQX435 induced PARP cleavage. AQX-435 effectively inhibits PI(3,4,5)P3-mediated signaling downstream of the BCR in CLL and DLBCL cells. AQX-435 and Ibrutinib combine effectively to enhanced inhibition of BCR signaling. AQX-435 induced TMD8 cell apoptosis in vitro with an IC50 of ~2 µM. AQX-435 reduces anti-IgM-induced AKT phosphorylation and induces apoptosis in DLBCL cells.
In Vivo:
AQX-435 (10 mg/kg; i.p.; 5 days) significantly reduced the volume of TMD8 tumors. AQX-435 (50 mg/kg; ip) inhibits DLBCL PDX tumors growth. AQX-435 reduced AKT phosphorylation and growth of DLBCL in vivo and cooperated with ibrutinib for tumor growth inhibition.
Products are for research use only. Not for human use.
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