Alternate TextTo enhance service speed and avoid tariff delays, we've opened a US warehouse. All US orders ship directly from our US facility.
Home > Products > Novel inhibitors

TAK-285

  Cat. No.:  DC7057   Featured
Chemical Structure
871026-44-7
For research use only. We do not sell to patients.
We match the best price and quality on market.
Email:order@dcchemicals.com  sales@dcchemicals.com
Tel:+86-021-58447131
Get Quotation Now
We are official vendor of:
  • 20
  • 19
  • 18
  • 17
  • 16
  • 15
  • 14
  • 12
  • 11
  • 10
  • 9
  • 8
  • 13
  • 6
  • 5
  • 4
  • 3
  • 2
  • 1
More than 5000 active chemicals with high quality for research!
Field of application
TAK-285 is a novel dual HER2 and EGFR(HER1) inhibitor with IC50 of 17 nM and 23 nM, >10-fold selectivity for HER1/2 than HER4, less potent to MEK1/5, c-Met, Aurora B, Lck, CSK etc.
Chemicals PropertiesBiological activity COAMSDSRelated productsDatasheet
Cas No.: 871026-44-7
Chemical Name: Tak-285
Synonyms: TAK 285;TAK-285;N-(2-(4-(3-Chloro-4-(3-(trifluoromethyl)phenoxy)phenylamino)-5H-pyrrolo[3,2-d]pyrimidin-5-yl)ethyl)-3-hydroxy-3-methylbutanamide;N-[2-[4-[3-chloro-4-[3-(trifluoromethyl)phenoxy]anilino]pyrrolo[3,2-d]pyrimidin-5-yl]ethyl]-3-hydroxy-3-methylbutanamide;03P;3poz;3rcd;n-(2-(4-((3-chloro-4-(3-(trifluoromethyl)phenoxy)phenyl)amino)-5h-pyrrolo(3,2-d)pyrimidin-5-yl)ethyl)-3-hydroxy-3-methylbutanamide;TAK285;70CCB438L6;N-{2-[4-({3-Chloro-4-[3-(Trifluoromethyl)phenoxy]phenyl}amino)-5h-Pyrrolo[3,2-D]pyrimidin-5-Yl]ethyl}-3-Hydroxy-3-Methylbutanamide;n-(2-(4-((3-chloro-4-(3-(trifluoromethyl)ph;N-[2-[4-[[3-Chloro-4-[3-(trifluoromethyl)phenoxy]phenyl]amino]-5H-pyrrolo[3,2-d]pyrimidin-5-yl]ethyl]-3-hydroxy-3-methylbutanamide (ACI);SDCCGSBI-0654472.P001;SDCCGSBI-0654472.P001;SDCCGSBI-0654472.P001;Q27265858;Q27265858;Q27265858;MLS006011276;MLS006011276;MLS006011276;N-(2-(4-((3-chloro-4-(3-(trifluoromethyl)phenoxy)phenyl)amino)-5H-pyrrolo[3,2-d]pyrimidin-5-yl)ethyl)-3-hydroxy-3-methylbutanamide;N-(2-(4-((3-chloro-4-(3-(trifluoromethyl)phenoxy)phenyl)amino)-5H-pyrrolo[3,2-d]pyrimidin-5-yl)ethyl)-3-hydroxy-3-methylbutanamide;N-(2-(4-((3-chloro-4-(3-(trifluoromethyl)phenoxy)phenyl)amino)-5H-pyrrolo[3,2-d]pyrimidin-5-yl)ethyl)-3-hydroxy-3-methylbutanamide;N-(2-{4-[3-chloro-4-(3-trifluoromethyl-phenoxy)-phenylamino]-pyrrolo[3,2-d]pyrimidin-5-yl}-ethyl)-3-hydroxy-3-methyl-butyramide;N-(2-{4-[3-chloro-4-(3-trifluoromethyl-phenoxy)-phenylamino]-pyrrolo[3,2-d]pyrimidin-5-yl}-ethyl)-3-hydroxy-3-methyl-butyramide;N-(2-{4-[3-chloro-4-(3-trifluoromethyl-phenoxy)-phenylamino]-pyrrolo[3,2-d]pyrimidin-5-yl}-ethyl)-3-hydroxy-3-methyl-butyramide;AKOS026674251;AKOS026674251;AKOS026674251;BCP04168;BCP04168;BCP04168;EX-A088;EX-A088;EX-A088;NSC800938;NSC800938;NSC800938;HY-15196;HY-15196;HY-15196;CCG-269993;CCG-269993;CCG-269993;AC-32052;AC-32052;AC-32052;TAK285/TAK-285;TAK285/TAK-285;TAK285/TAK-285;BDBM50358430;BDBM50358430;BDBM50358430;J-522793;J-522793;J-522793;BRD-K80343549-001-02-6;BRD-K80343549-001-02-6;BRD-K80343549-001-02-6;SB19365;SB19365;SB19365;871026-44-7;871026-44-7;871026-44-7;DB-361054;DB-361054;DB-361054;HMS3750E17;HMS3750E17;HMS3750E17;EGFR/HER2 Kinase Inhibitor TAK-285;EGFR/HER2 Kinase Inhibitor TAK-285;EGFR/HER2 Kinase Inhibitor TAK-285;CHEMBL1614725;CHEMBL1614725;CHEMBL1614725;DTXCID10158627;DTXCID10158627;DTXCID10158627;3w2o;3w2o;3w2o;BCP0726000091;BCP0726000091;BCP0726000091;UNII-70CCB438L6;UNII-70CCB438L6;UNII-70CCB438L6;SCHEMBL982278;SCHEMBL982278;SCHEMBL982278;NCGC00346699-06;NCGC00346699-06;NCGC00346699-06;AS-16291;AS-16291;AS-16291;NCGC00346699-01;NCGC00346699-01;NCGC00346699-01;TAK 285 [WHO-DD];TAK 285 [WHO-DD];TAK 285 [WHO-DD];SMR004703026;SMR004703026;SMR004703026;SW219902-1;SW219902-1;SW219902-1;N-(2-(4-(3-CHLORO-4-(3-(TRIFLUOROMETHYL)PHENOXY)PHENYLAMINO)-5H-PYRROLO[3,2-D]PYRIMIDIN-5-YL)ETHYL)-3-HYDROXY-3-METHYLBUTANAMIDE;...
SMILES: O=C(CC(C)(C)O)NCCN1C2C(=NC=NC=2NC2C=C(Cl)C(OC3C=C(C(F)(F)F)C=CC=3)=CC=2)C=C1
Formula: C26H25ClF3N5O3
M.Wt: 547.956615209579
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: Among the 34 kinases tested, TAK-285 only significantly inhibits HER4 with IC50 of 260 nM, slightly inhibits MEK1, MEK5, c-Met, Aurora B, Lck, CSK, and Lyn B with IC50 of 1.1 μM, 5.7 μM, 4.2 μM, 1.7 μM, 2.4 μM, 4.7 μM, and 5.2 μM, respectively, and displays no activity against other kinases with IC50 of >10 μM. TAK-285 shows significant growth inhibitory activity against BT-474 cells (HER2-overexpressing human breast cancer cell line) with GI50 of 17 nM. Compared with SYR127063 a potent inhibitor of HER2, TAK-285 displays similar in vitro potency against HER2 and EGFR. Compared with the full cytoplasmic domains of the wild-type proteins, the mutations and shortened boundaries used For structure determination of HER2-KD and EGFR-KD do not significantly change the inhibitory activity (IC50) of TAK-285. TAK-285 binds to the inactive con Formation of EGFR, and shows a similar binding mode with lapatinib in the active site. The oral bioavailability of TAK-285 is 97.7% in rats and 72.2% in mice at a dose of 50 mg/kg. Oral administration of TAK-285 at 100 mg/kg twice daily For 14 days displays significant antitumor efficacy in the HER2-overexpressing BT-474 tumor xenograft mouse model with tumor/control (T/C) ratio of 29%, without affecting body weight. Similar to the BT-474 model, TAK-285 exhibits dose-dependent tumor growth inhibition of 4-1ST (HER2-overexpressing human gastric cancer tumor) xenografts in mice, with T/C of 44% and 11% at doses of 50 mg/kg and 100 mg/kg, twice daily, respectively, without significant body weight loss in mice. Furthermore, TAK-285 treatment induces dose-dependent growth inhibition of 4-1ST tumors in rats with T/C of 38% and 14% at doses of 6.25 mg/kg and 12.5 mg/kg, and, particularly noteworthy, tumor regression with T/C of -12% and -16% at doses of 25 mg/kg and 50 mg/kg, respectively. After oral administration of TAK-285, a significant amount of TAK-285 is present in the brain of rats in pharmacologically active, unbound Form (approximately 20% of its free plasma level), indicating that TAK-285 has a potential in the therapy of CNS malignancies/metastases. For the detailed information of TAK-285, the solubility of TAK-285 in water, the solubility of TAK-285 in DMSO, the solubility of TAK-285 in PBS buffer, the animal experiment (test) of TAK-285, the cell expriment (test) of TAK-285, the in vivo, in vitro and clinical trial test of TAK-285, the EC50, IC50,and Affinity of TAK-285, Please contact DC Chemicals.
COA
MSDS
Cat. No. Product name Field of application
DC57050 DZD9008 DZD9008 is an oral, potent, irreversible, wild type-selective EGFR TKI against EGFR or HER2 Exon20ins and other mutations.
DC74400 OBX02-011 OBX02-011 is a potent, reversible, fourth-generation EGFR tyrosine kinase inhibitor (TKI) that overcomes the EGFR C797S mutation, inhibits triple mutants Del19/T790M/C797S and L858R/T790M/C797S with IC50 of 0.134 and 2.09 nM, respectively.
DC74398 HSL119 HSL119 is a highly effective and selective inhibitor of hormonally upregulated neu-associated kinase (HUNK), demonstrating complete suppression of HUNK kinase activity at a concentration of 1 µM in biochemical assays. This compound highlights its precision and potency in targeting HUNK.
DC74394 DSF-102 DSF-102 (DSF102) is a small molecule EGFR inhibitor that interacts with the extracellular domain (ECD) of EGFR, inhibits the interaction with the EGF instead of blocking the intracellular kinase activity, shows inhibition of EGFR dimerization with IC50 of
DC74393 BI-8128 BI-8128 is a potent, selective, reversible and orally bioavailable fourth generation EGFR inhibitor, potently inhibits oncogenic EGFR variants del19 and L858R as well as the acquired EGFR resistance mutations T790M and C797S.
DC70170 AC3573 AC3573 (AC-3573) is a potent, specific small molecule inhibitor of HER3.AC3573 abrogates HER2–HER3 signalling in cells and is more specific for HER3, inhibits NRG (heregulin)-induced HER3 phosphorylation with IC50 of 10 uM, abrogates the formation of the active HER2-HER3 heterodimer, inhibits oncogenic downstream signalling in SK-BR-3 breast cancer cells.
DC46930 Sunvozertinib Sunvozertinib is a potent inhibitor targeting the ErbB family of receptor tyrosine kinases, including EGFR (Epidermal Growth Factor Receptor) and Her2 (Human Epidermal Growth Factor Receptor 2), as well as BTK (Bruton's Tyrosine Kinase). It exhibits particularly strong activity against mutant forms of these kinases, which are often associated with resistance to existing therapies in cancers such as non-small cell lung cancer (NSCLC). The IC50 values (half-maximal inhibitory concentr.
DC46163 Epitinib Epitinib is an orally active and selective epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI) designed for optimal brain penetration. Epitinib can be used for the research of cancer.
DC45794 Tucatinib hemiethanolate Tucatinib (Irbinitinib) hemiethanolate is a potent, orally active and selective HER2 inhibitor with an IC50 of 8 nM.
DC45317 EGFR/ErbB-2/ErbB-4 inhibitor-2 EGFR/ErbB-2/ErbB-4 inhibitor-2 (Compound 5) is a EGFR and ErbB inhibitor with IC50s of 0.017 μM, 0.08 μM, 1.91 μM.
X
Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.
Site Map|Privacy PolicyCopyright © 2018-2020 All Rights Reserved. Technical Support:KuuJia