Description
ASTX660 is an orally bioavailable dual antagonist of cellular inhibitor of apoptosis protein (cIAP) and X-linked inhibitor of apoptosis protein (XIAP).
Product information
CAS Number: 1799328-86-1
Molecular Weight: 539.68
Formula: C30H42FN5O3
Chemical Name: 1-{6-[(4-fluorophenyl)methyl]-5-(hydroxymethyl)-3,3-dimethyl-1H,2H,3H-pyrrolo[3,2-b]pyridin-1-yl}-2-[(2R,5R)-5-methyl-2-{[(3R)-3-methylmorpholin-4-yl]methyl}piperazin-1-yl]ethan-1-one
Smiles: C[C@@H]1CN(CC(=O)N2CC(C)(C)C3=NC(CO)=C(CC4C=CC(F)=CC=4)C=C23)[C@@H](CN2CCOC[C@H]2C)CN1
InChiKey: YCXOHEXZVKOGEV-DNRQZRRGSA-N
InChi: InChI=1S/C30H42FN5O3/c1-20-14-35(25(13-32-20)15-34-9-10-39-18-21(34)2)16-28(38)36-19-30(3,4)29-27(36)12-23(26(17-37)33-29)11-22-5-7-24(31)8-6-22/h5-8,12,20-21,25,32,37H,9-11,13-19H2,1-4H3/t20-,21-,25-/m1/s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 100 mg/mL (185.29 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:
ASTX660 is an orally bioavailable dual antagonist of cIAP and XIAP, currently being investigated in a single-agent Phase 1/2 clinical trial in patients with advanced solid tumors and lymphomas. Twenty-one triple-negative breast cancer (TNBC) cell lines are treated with ASTX660 in vitro and it is found that 43% are sensitive to ASTX660.
In Vivo:
In HCC1806 xenografts in mice, ASTX660 (daily oral treatment) causes moderate tumor growth inhibition but not regression.
Products are for research use only. Not for human use.
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