Product Name :
Tarloxotinib bromide
Description:
Tarloxotinib bromide (TH-4000) is an irreversible EGFR/HER2 inhibitor.
CAS:
1636180-98-7
Molecular Weight:
681.77
Formula:
C24H24Br2ClN9O3
Chemical Name:
[(2E)-3-(4-[(3-bromo-4-chlorophenyl)amino]pyrido[3,4-d]pyrimidin-6-ylcarbamoyl)prop-2-en-1-yl]dimethyl[(1-methyl-4-nitro-1H-imidazol-5-yl)methyl]azanium bromide
Smiles :
[Br-].CN1C=NC(=C1C[N+](C)(C)C/C=C/C(=O)NC1=CC2C(NC3C=CC(Cl)=C(Br)C=3)=NC=NC=2C=N1)[N+]([O-])=O
InChiKey:
WAKIMVYUBWMMHJ-FXRZFVDSSA-N
InChi :
InChI=1S/C24H23BrClN9O3.BrH/c1-33-14-30-24(34(37)38)20(33)12-35(2,3)8-4-5-22(36)32-21-10-16-19(11-27-21)28-13-29-23(16)31-15-6-7-18(26)17(25)9-15;/h4-7,9-11,13-14H,8,12H2,1-3H3,(H-,27,28,29,31,32,36);1H/b5-4+;
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.
Additional information:
Tarloxotinib bromide (TH-4000) is an irreversible EGFR/HER2 inhibitor.|Product information|CAS Number: 1636180-98-7|Molecular Weight: 681.77|Formula: C24H24Br2ClN9O3|Chemical Name: [(2E)-3-(4-[(3-bromo-4-chlorophenyl)amino]pyrido[3,4-d]pyrimidin-6-ylcarbamoyl)prop-2-en-1-yl]dimethyl[(1-methyl-4-nitro-1H-imidazol-5-yl)methyl]azanium bromide|Smiles: [Br-].CN1C=NC(=C1C[N+](C)(C)C/C=C/C(=O)NC1=CC2C(NC3C=CC(Cl)=C(Br)C=3)=NC=NC=2C=N1)[N+]([O-])=O|InChiKey: WAKIMVYUBWMMHJ-FXRZFVDSSA-N|InChi: InChI=1S/C24H23BrClN9O3.BrH/c1-33-14-30-24(34(37)38)20(33)12-35(2,3)8-4-5-22(36)32-21-10-16-19(11-27-21)28-13-29-23(16)31-15-6-7-18(26)17(25)9-15;/h4-7,9-11,13-14H,8,12H2,1-3H3,(H-,27,28,29,31,32,36);1H/b5-4+;|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: DMSO : ≥ 33 mg/mL (48.SNPB ADC Linker 40 mM).Toremifene Epigenetic Reader Domain |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.PMID:32552230 |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:|To confirm the mechanism of action, Tarloxotinib bromide is shown to be metabolized efficiently under hypoxia using a panel of human NSCLC cell lines (rate of TKI release 0.4-2.1 nM/hr/106 cells), a process that is inhibited by oxygen (TKI release 80% (538 vs 99 nM/kg; pIn Vivo:|A prototypic WT EGFR driven xenograft model (A431) is used to benchmark Tarloxotinib bromide activity against each EGFR-TKI by “retrotranslation” of reported plasma exposure for each agent in human subjects back to the xenograft model. Only treatment with clinically relevant doses and schedules of Tarloxotinib bromide is associated with tumor regression and durable inhibition of WT EGFR tumor phosphorylation. Consistent with these findings, Tarloxotinib bromide treatment can also regress the WT EGFR NSCLC tumor models H125 and H1648, demonstrating Tarloxotinib bromide provides the necessary therapeutic index to inhibit WT EGFR in vivo.|Products are for research use only. Not for human use.|
