Description
ONX 0801 (BGC 945) trisodium is a thymidylate synthase (TS) inhibitor, targeted to α-folate receptor–overexpressing tumors.
Product information
CAS Number: 1097638-00-0
Molecular Weight: 713.58
Formula: C32H30N5Na3O10
Chemical Name: trisodium (2R)-2-[(4S)-4-carboxylato-4-[(4-{[(6S)-2-(hydroxymethyl)-4-oxo-3H,4H,6H,7H,8H-cyclopenta[g]quinazolin-6-yl](prop-2-yn-1-yl)amino}phenyl)formamido]butanamido]pentanedioate
Smiles: [Na+].[Na+].[Na+].C#CCN([C@H]1CCC2=CC3N=C(CO)NC(=O)C=3C=C21)C1C=CC(=CC=1)C(=O)N[C@@H](CCC(=O)N[C@H](CCC([O-])=O)C([O-])=O)C([O-])=O
InChiKey: JMUBAMVCKZFETQ-GVNLSHJKSA-K
InChi: InChI=1S/C32H33N5O10.3Na/c1-2-13-37(25-10-5-18-14-24-21(15-20(18)25)30(43)36-26(16-38)33-24)19-6-3-17(4-7-19)29(42)35-23(32(46)47)8-11-27(39)34-22(31(44)45)9-12-28(40)41;;;/h1,3-4,6-7,14-15,22-23,25,38H,5,8-13,16H2,(H,34,39)(H,35,42)(H,40,41)(H,44,45)(H,46,47)(H,33,36,43);;;/q;3*+1/p-3/t22-,23+,25+;;;/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:
ONX 0801 (BGC 945) is designed to further reduce toxicity by more effectively targeting cancer cells that overexpress the α-FR. ONX 0801 (BGC 945) exhibits IC50 values of of 6.6 μM, 1.1 nM, 3.3 nM, 90 nM and 0.32 μM in A431, A431-FBP, KB, IGROV-1 and JEG-3 cells.
In Vivo:
BGC 945 (100 mg/kg, ip/iv injection) in the tumor had a longer half-life (28 hours) compared with other tissues. BGC 945 (100 mg/kg daily for 16 days) does not lead to body weight loss, macroscopic signs of toxicity to the major organs, or a change in renal function. BGC 945 at 100mg/kg induces a 5-20-fold increase in tumor dUrd at 4-72h without increases in the plasma, consistent with tumor targeting.
Products are for research use only. Not for human use.
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