Name: BLU9931
CAS#: 1538604-68-0
Chemical Formula: C26H22Cl2N4O3
Exact Mass: 508.1069
Molecular Weight: 509.38
Elemental Analysis: C, 61.31; H, 4.35; Cl, 13.92; N, 11.00; O, 9.42
EOS Med Chem produce BLU9931, 1538604-68-0 in GMP plant, C-GMP standard, now COA, NMR, HPLC, MS is ok.
BLU9931, 1538604-68-0 Intermediates, EOS Med Chem have 8; BLU9931, 1538604-68-0 Impurity we have 10, all from GMP, FDA plant.
Now BLU9931, 1538604-68-0 DMF document is preparing.
Until 2016, Aug, BLU9931, 1538604-68-0 more than produced 25kg API, 120kg Intermediates
BLU-9931 Intermediates 6-(2,6-dichloro-3,5-dimethoxyphenyl)-N-(2-methyl-6-nitrophenyl)quinazolin-2-amine 1538605-09-2
GMP PRODUCE:
Alectinib;Veliparib;Acalabrutinib;Venetoclax;Sotagliflozin;Ledipasvir;LX1606;Anacetrapib;Abemaciclib
Description: BLU9931 is a potent and irreversible small-molecule inhibitor of FGFR4, as a targeted therapy to treat patients with HCC whose tumors have an activated FGFR4 signaling pathway. BLU9931 is exquisitely selective for FGFR4 versus other FGFR family members and all other kinases. BLU9931 shows remarkable antitumor activity in mice bearing an HCC tumor xenograft that overexpresses FGF19 due to amplification as well as a liver tumor xenograft that overexpresses FGF19 mRNA but lacks FGF19 amplification. Approximately one third of patients with HCC whose tumors express FGF19 together with FGFR4 and its coreceptor klotho β (KLB) could potentially respond to treatment with an FGFR4 inhibitor.
Synonym: BLU9931; BLU-9931; BLU 9931.
IUPAC/Chemical Name: N-(2-((6-(2,6-dichloro-3,5-dimethoxyphenyl)quinazolin-2-yl)amino)-3-methylphenyl)acrylamide
SMILES Code: C=CC(NC1=CC=CC(C)=C1NC2=NC=C3C=C(C4=C(Cl)C(OC)=CC(OC)=C4Cl)C=CC3=N2)=O
1: Packer LM, Pollock PM. Paralog-Specific Kinase Inhibition of FGFR4: Adding to the Arsenal of Anti-FGFR Agents. Cancer Discov. 2015 Apr;5(4):355-7. doi: 10.1158/2159-8290.CD-15-0246. PubMed PMID: 25847957.
2: Hagel M, Miduturu C, Sheets M, Rubin N, Weng W, Stransky N, Bifulco N, Kim JL, Hodous B, Brooijmans N, Shutes A, Winter C, Lengauer C, Kohl NE, Guzi T. First Selective Small Molecule Inhibitor of FGFR4 for the Treatment of Hepatocellular Carcinomas with an Activated FGFR4 Signaling Pathway. Cancer Discov. 2015 Apr;5(4):424-37. doi: 10.1158/2159-8290.CD-14-1029. Epub 2015 Mar 16. PubMed PMID: 25776529.
CAS#: 1538604-68-0
Chemical Formula: C26H22Cl2N4O3
Exact Mass: 508.1069
Molecular Weight: 509.38
Elemental Analysis: C, 61.31; H, 4.35; Cl, 13.92; N, 11.00; O, 9.42
EOS Med Chem produce BLU9931, 1538604-68-0 in GMP plant, C-GMP standard, now COA, NMR, HPLC, MS is ok.
BLU9931, 1538604-68-0 Intermediates, EOS Med Chem have 8; BLU9931, 1538604-68-0 Impurity we have 10, all from GMP, FDA plant.
Now BLU9931, 1538604-68-0 DMF document is preparing.
Until 2016, Aug, BLU9931, 1538604-68-0 more than produced 25kg API, 120kg Intermediates
BLU-9931 Intermediates 6-(2,6-dichloro-3,5-dimethoxyphenyl)-N-(2-methyl-6-nitrophenyl)quinazolin-2-amine 1538605-09-2
GMP PRODUCE:
Alectinib;Veliparib;Acalabrutinib;Venetoclax;Sotagliflozin;Ledipasvir;LX1606;Anacetrapib;Abemaciclib
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Description: BLU9931 is a potent and irreversible small-molecule inhibitor of FGFR4, as a targeted therapy to treat patients with HCC whose tumors have an activated FGFR4 signaling pathway. BLU9931 is exquisitely selective for FGFR4 versus other FGFR family members and all other kinases. BLU9931 shows remarkable antitumor activity in mice bearing an HCC tumor xenograft that overexpresses FGF19 due to amplification as well as a liver tumor xenograft that overexpresses FGF19 mRNA but lacks FGF19 amplification. Approximately one third of patients with HCC whose tumors express FGF19 together with FGFR4 and its coreceptor klotho β (KLB) could potentially respond to treatment with an FGFR4 inhibitor.
Synonym: BLU9931; BLU-9931; BLU 9931.
IUPAC/Chemical Name: N-(2-((6-(2,6-dichloro-3,5-dimethoxyphenyl)quinazolin-2-yl)amino)-3-methylphenyl)acrylamide
SMILES Code: C=CC(NC1=CC=CC(C)=C1NC2=NC=C3C=C(C4=C(Cl)C(OC)=CC(OC)=C4Cl)C=CC3=N2)=O
1: Packer LM, Pollock PM. Paralog-Specific Kinase Inhibition of FGFR4: Adding to the Arsenal of Anti-FGFR Agents. Cancer Discov. 2015 Apr;5(4):355-7. doi: 10.1158/2159-8290.CD-15-0246. PubMed PMID: 25847957.
2: Hagel M, Miduturu C, Sheets M, Rubin N, Weng W, Stransky N, Bifulco N, Kim JL, Hodous B, Brooijmans N, Shutes A, Winter C, Lengauer C, Kohl NE, Guzi T. First Selective Small Molecule Inhibitor of FGFR4 for the Treatment of Hepatocellular Carcinomas with an Activated FGFR4 Signaling Pathway. Cancer Discov. 2015 Apr;5(4):424-37. doi: 10.1158/2159-8290.CD-14-1029. Epub 2015 Mar 16. PubMed PMID: 25776529.
