BLU9931
Catalog No: 60303
CAS Number: 1538604-68-0
Purity: 98%
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 (KLB) could potentially respond to treatment with an FGFR4 inhibitor. These findings are the first demonstration of a therapeutic strategy that targets a subset of patients with HCC.
Cancer Discov; 5(4); 424-37. ©2015 AACR. See related commentary by Packer and Pollock, p. 355 This article is highlighted in the In This Issue feature, p. 333.
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 (KLB) could potentially respond to treatment with an FGFR4 inhibitor. These findings are the first demonstration of a therapeutic strategy that targets a subset of patients with HCC.
Cancer Discov; 5(4); 424-37. ©2015 AACR. See related commentary by Packer and Pollock, p. 355 This article is highlighted in the In This Issue feature, p. 333.
©2015 American Association for Cancer Research.
For research use only. We do not sell to patients.
Chemical Information
| Name | BLU9931 |
|---|---|
| Iupac Chemical Name | N-(2-((6-(2,6-dichloro-3,5-dimethoxyphenyl)quinazolin-2-yl)amino)-3-methylphenyl)acrylamide |
| Molecular Formula | C26H22Cl2N4O3 |
| Molecular Weight | 509.38 |
| Smile | C=CC(NC1=CC=CC(C)=C1NC2=NC=C3C=C(C4=C(Cl)C(OC)=CC(OC)=C4Cl)C=CC3=N2)=O |
| InChiKey | TXEBNKKOLVBTFK-UHFFFAOYSA-N |
| InChi | InChI=1S/C26H22Cl2N4O3/c1-5-21(33)30-18-8-6-7-14(2)25(18)32-26-29-13-16-11-15(9-10-17(16)31-26)22-23(27)19(34-3)12-20(35-4)24(22)28/h5-13H,1H2,2-4H3,(H,30,33)(H,29,31,32) |
| CAS Number | 1538604-68-0 |
| Related CAS |
Ordering Information
| Packaging | Price | Availability | Purity | Shipping Time |
|---|---|---|---|---|
| Bulk | Enquiry | Enquiry | Enquiry |
| Formulation | crystalline solid |
|---|---|
| Purity | 98% |
| Storage | 3 years -20ºCpowder |
| Solubility | Soluble in DMSO |
| Handling | |
| Shipping Condition | Shipped under ambient temperature as non-hazardous chemical. |
| HS Code |
Coming soon.
| Targets | |
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| Mechanism | |
| Cell study | |
| Animal study | |
| Clinical study |
Not available
Chemical Structure
