TAK-285|TAK285 HER inhibitor|DC Chemicals|Price|Buy

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.

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2018-0101

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.
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
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.
DC41015	BDTX-189	BDTX-189 is a potent, orally active and selective inhibitor of allosteric EGFR and HER2 oncogenic mutations, includes EGFR/HER2 exon 20 insertion mutants. BDTX-189 shows KDs of 0.2, 0.76, 13 and 1.2 nM for EGFR, HER2, BLK and RIPK2, reapectively. Anticancer activity.
DC28953	Mobocertinib(TAK-788)	Mobocertinib is a epidermal growth factor receptor (EGFR) inhibitor and an antineoplastic.
DC28949	JBJ-04-125-02	JBJ-04-125-02 is a potent, mutant-selective, allosteric and orally active EGFR inhibitor with an IC50 of 0.26 nM for EGFRL858R/T790M. JBJ-04-125-02 can inhibit cancer cell proliferation and EGFRL858R/T790M/C797S signaling. JBJ-04-125-02 has anti-tumor activities.
DC8557	AG879	Tyrphostin AG 879 is a protein tyrosine kinase inhibitor with potent effects on TrkA.
DC7057	TAK-285	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.