Mubritinib - CAS 366017-09-6
Catalog number: B0084-067201
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C25H23F3N4O2
Molecular Weight:
468.48
COA:
Inquire
Targets:
EGFR
Description:
Mubritinib, also known as TAK-165, is a protein kinase inhibitor which was under development by Takeda for the treatment of cancer. It completed phase I clinical trials (may be discontinued since 2008). Mubritinib(TAK 165) is a potent EGFR, HER2 and p34cdc2 inhibitor with IC50 of 6 nM and 0.2 µM, respectively. Mubritinib(TAK 165) also inhibits p33cdk2 and p33cdk5. Mubritinib(TAK 165) displays > 4000-fold selectivity over EGFR, FGFR, PDGFR, JAK1 and Src. Mubritinib(TAK 165) exhibits potent antiproliferative effects in ErbB2-overexpressing cancer cell lines (IC50 = 5 nM in BT474 breast cancer cells) and significantly inhibits bladder, breast and prostate cancer xenograft growth in vivo.
Ordering Information
Catalog Number Size Price Stock Quantity
B0084-067201 50 mg $168 In stock
B0084-067201 100 mg $298 In stock
Bulk Inquiry
Purity:
0.98
Appearance:
white solid powder
Synonyms:
Mubritinib; TAK165; TAK-165; TAK-165
MSDS:
Inquire
InChIKey:
ZTFBIUXIQYRUNT-MDWZMJQESA-N
InChI:
InChI=1S/C25H23F3N4O2/c26-25(27,28)21-9-4-20(5-10-21)8-13-24-30-22(18-34-24)17-33-23-11-6-19(7-12-23)3-1-2-15-32-16-14-29-31-32/h4-14,16,18H,1-3,15,17H2/b13-8+
Canonical SMILES:
C1=CC(=CC=C1CCCCN2C=CN=N2)OCC3=COC(=N3)C=CC4=CC=C(C=C4)C(F)(F)F
Current Developer:
Takeda, Japan.
1.miR-125a regulates cell cycle, proliferation, and apoptosis by targeting the ErbB pathway in acute myeloid leukemia.
Ufkin ML1, Peterson S1, Yang X2, Driscoll H3, Duarte C2, Sathyanarayana P4. Leuk Res. 2014 Mar;38(3):402-10. doi: 10.1016/j.leukres.2013.12.021. Epub 2014 Jan 8.
microRNA profiling of acute myeloid leukemia patient samples identified miR-125a as being decreased. Current literature has investigated miR-125a's role in normal hematopoiesis but not within acute myeloid leukemia. Analysis of the upstream region of miR-125a identified several CpG islands. Both precursor and mature miR-125a increased in response to a de-methylating agent, Decitabine. Profiling revealed the ErbB pathway as significantly decreased with ectopic miR-125a. Either ectopic expression of miR-125a or inhibition of ErbB via Mubritinib resulted in inhibition of cell cycle proliferation and progression with enhanced apoptosis revealing ErbB inhibitors as potential novel therapeutic agents for treating miR-125a-low AML.
2.Epithelial-mesenchymal transition confers resistance to selective FGFR inhibitors in SNU-16 gastric cancer cells.
Grygielewicz P1,2, Dymek B3, Bujak A3,4, Gunerka P3,5, Stanczak A3, Lamparska-Przybysz M3, Wieczorek M3, Dzwonek K3,6, Zdzalik D3. Gastric Cancer. 2016 Jan;19(1):53-62. doi: 10.1007/s10120-014-0444-1. Epub 2014 Nov 19.
BACKGROUND: Up to 10 % of primary gastric cancers are characterized by FGFR2 amplification, and fibroblast growth factor receptor (FGFR) inhibitors may represent therapeutic agents for patients with these malignancies. However, long-term benefits of the treatment might be limited owing to the occurrence of drug resistance.
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related EGFR Products


CAS 194423-15-9 PD-168393

PD-168393
(CAS: 194423-15-9)

PD-168393 is a potent, cell-permeable, irreversible, ATP-competitive and selective inhibitor of EGF receptor (EGFR) tyrosine kinase activity (IC50 = 700 pM). It...

BMS 599626 dihydrochloride

BMS 599626 dihydrochloride is a potent and selective EGFR and ErbB2 inhibitor (IC50 = 22 nM and 32 nM, respectively), and also inhibits HER4 (IC50 = 190 nM). BM...

CAS 937265-83-3 ARRY-380

ARRY-380
(CAS: 937265-83-3)

ARRY-380 is a potent and selective HER2 inhibitor with IC50 of 8 nM, equipotent against truncated p95-HER2, 500-fold more selective for HER2 versus EGFR.

CAS 1050500-29-2 AST-1306

AST-1306
(CAS: 1050500-29-2)

AST-1306 is a novel irreversible inhibitor of EGFR and ErbB2 with IC50 of 0.5 nM and 3 nM, also effective in mutation EGFR T790M/L858R, more potent to ErbB2-ove...

CGP-59326
(CAS: 173458-56-5)

CGP-59326, a pyrrolopyrimidine derivative, has been found to be an EGFR antagonist and could used in antineoplastic studies.

MTX-211
(CAS: 1952236-05-3)

MTX-211 is a dual inhibitor of EGFR and PI3K, which plays important roles in the progression of KRAS mutant colorectal cancer. MTX-211 has the potential for the...

CAS 171179-06-9 PD158780

PD158780
(CAS: 171179-06-9)

PD158780 is a potent, cell-permeable, reversible ATP-competitive inhibitor of EGFR tyrosine kinase activity with IC50 values of 0.008, 49 and 52 nM for EGFR, Er...

CO-1686 hydrobromide
(CAS: 1446700-26-0)

CO-1686 hydrobromide is the hydrobromide salt form of CO-1686. CO-1686, also called as Rociletinib, is an oral tyrosine kinase inhibitor that irreversibly and s...

Chemical Structure

CAS 366017-09-6 Mubritinib

Quick Inquiry

Verification code

Featured Items