Product Name :
Mobocertinib succinate
Description:
Mobocertinib succinate (TAK-788 succinate) is a potent and orally active inhibitor of EGFR and HER2 oncogenic mutants, including exon 20 insertions, with selectivity over WT EGFR. Antitumor activity.
CAS:
2389149-74-8
Molecular Weight:
703.78
Formula:
C36H45N7O8
Chemical Name:
butanedioic acid; propan-2-yl 2-[(4-{[2-(dimethylamino)ethyl](methyl)amino}-2-methoxy-5-(prop-2-enamido)phenyl)amino]-4-(1-methyl-1H-indol-3-yl)pyrimidine-5-carboxylate
Smiles :
CN(C)CCN(C)C1=CC(OC)=C(C=C1NC(=O)C=C)NC1=NC(=C(C=N1)C(=O)OC(C)C)C1=CN(C)C2=CC=CC=C12.OC(=O)CCC(O)=O
InChiKey:
YXYAEUMTJQGKHS-UHFFFAOYSA-N
InChi :
InChI=1S/C32H39N7O4.C4H6O4/c1-9-29(40)34-24-16-25(28(42-8)17-27(24)38(6)15-14-37(4)5)35-32-33-18-22(31(41)43-20(2)3)30(36-32)23-19-39(7)26-13-11-10-12-21(23)26;5-3(6)1-2-4(7)8/h9-13,16-20H,1,14-15H2,2-8H3,(H,34,40)(H,33,35,36);1-2H2,(H,5,6)(H,7,8)
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.{{Tolvaptan} site|{Tolvaptan} GPCR/G Protein|{Tolvaptan} Technical Information|{Tolvaptan} Data Sheet|{Tolvaptan} supplier|{Tolvaptan} Autophagy}
Additional information:
Mobocertinib succinate (TAK-788 succinate) is a potent and orally active inhibitor of EGFR and HER2 oncogenic mutants, including exon 20 insertions, with selectivity over WT EGFR. Antitumor activity.|Product information|CAS Number: 2389149-74-8|Molecular Weight: 703.78|Formula: C36H45N7O8|Chemical Name: butanedioic acid; propan-2-yl 2-[(4-{[2-(dimethylamino)ethyl](methyl)amino}-2-methoxy-5-(prop-2-enamido)phenyl)amino]-4-(1-methyl-1H-indol-3-yl)pyrimidine-5-carboxylate|Smiles: CN(C)CCN(C)C1=CC(OC)=C(C=C1NC(=O)C=C)NC1=NC(=C(C=N1)C(=O)OC(C)C)C1=CN(C)C2=CC=CC=C12.OC(=O)CCC(O)=O|InChiKey: YXYAEUMTJQGKHS-UHFFFAOYSA-N|InChi: InChI=1S/C32H39N7O4.C4H6O4/c1-9-29(40)34-24-16-25(28(42-8)17-27(24)38(6)15-14-37(4)5)35-32-33-18-22(31(41)43-20(2)3)30(36-32)23-19-39(7)26-13-11-10-12-21(23)26;5-3(6)1-2-4(7)8/h9-13,16-20H,1,14-15H2,2-8H3,(H,34,40)(H,33,35,36);1-2H2,(H,5,6)(H,7,8)|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: DMSO : 25 mg/mL (35.{{Streptavidin Protein} MedChemExpress|{Streptavidin Protein} Protocol|{Streptavidin Protein} Purity|{Streptavidin Protein} custom synthesis|{Streptavidin Protein} Epigenetics} 52 mM; Need ultrasonic).PMID:33215805 |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:|Mobocertinib succinate (TAK-788 succinate) inhibits all 14 mutant variants of EGFR (IC50s=2.4-22 nM), and all 6 mutant variants of HER2 (IC50s=2.4-26 nM), more potently than it inhibited WT EGFR (IC50=35 nM), including all 8 variants with exon 20 activating insertions.|In Vivo:|In mice implanted with a patient-derived tumor containing an EGFR exon 20 activating insertion, or with engineered Ba/F3 cells containing a HER2 exon 20 activating insertion, once daily oral dosing of Mobocertinib succinate induced regression of tumors at doses that were well tolerated (30-100 mg/kg).|Products are for research use only. Not for human use.|
