TAK-285 is a novel dual erbB protein kinase inhibitor that specifically targets human epidermal growth factor receptor (EGFR) and HER2. Methods: TAK-285 is currently being developed by Takeda. TAK-285 was found to be well tolerate in Phase I trials. Absorption of TAK-285 was rapid after oral dosing, and plasma exposure at steady-state increased in a dose-proportional fashion for doses ranging from 50 to 300 mg b.i.d. A partial response was observed for one patient with parotid cancer who received 300 mg b.i.d. The toxicity profile and PK properties of oral TAK-285 warrant further evaluation.

June 21, 2017

prudect name : TAK-285 is a novel dual erbB protein kinase inhibitor that specifically targets human epidermal growth factor receptor (EGFR) and HER2. Methods: TAK-285 is currently being developed by…

๐Ÿ“Œ
0๐Ÿ’ฌ read more

prudect name : Torin 1Synonyms: Torin 1CAS NO: 1222998-36-8Molecular Formula: C35H28F3N5O2Molecular Weight: 607.62Purity: 98% minSolubility:

prudect name : Torin 1 Synonyms: Torin 1CAS NO: 1222998-36-8Molecular Formula: C35H28F3N5O2Molecular Weight: 607.62Purity: 98% minSolubility: In DMSOStorage: −20°C web site: www.medchemexpress.com

๐Ÿ“Œ
0๐Ÿ’ฌ read more

Tofacitinib inhibits IL-2-mediated human T cell blast proliferation and IL-15-induced CD69 expression with IC50 of 11 nM and 48 nM, respectively. Tofacitinib prevents mixed lymphocyte reaction with IC50 of 87 nM. Tofacitinib treatment of murine factor-dependent cell PatersenยจCerythropoietin receptor (FDCP-EpoR) cells harboring human wild-type or V617F JAK2 leads to prevention of cell proliferation with IC50 of 2.1 µM and 0.25 µM, respectively. Tofacitinib inhibits interleukin-6-induced phosphorylation of STAT1 and STAT3 with IC50 of 23 nM and 77 nM, respectively. Moreover, Tofacitinib generates a significant pro-apoptotic effect on murine FDCP-EpoR cells carrying JAK2VV617F, whereas a lesser effect was observed for cells carrying wild-type JAK2. This activity is coupled with the inhibition of phosphorylation of the key JAK2V617F-dependent downstream signaling effectors signal transducer and activator of transcription (STAT)3, STAT5, and v-akt murine thymoma viral oncogene homolog (AKT).

prudect name : Tofacitinib inhibits IL-2-mediated human T cell blast proliferation and IL-15-induced CD69 expression with IC50 of 11 nM and 48 nM, respectively. Tofacitinib prevents mixed lymphocyte reaction with…

๐Ÿ“Œ
0๐Ÿ’ฌ read more

prudect name : THIACETAZONESynonyms: CAS NO: 104-06-3Molecular Formula: C10H12N4OSMolecular Weight: 236.29Purity: 98% minSolubility: In DMSOStorage:

prudect name : THIACETAZONE Synonyms: CAS NO: 104-06-3Molecular Formula: C10H12N4OSMolecular Weight: 236.29Purity: 98% minSolubility: In DMSOStorage: -20°C web site: www.medchemexpress.com

๐Ÿ“Œ
0๐Ÿ’ฌ read more

prudect name : Terbinafine hydrochlorideSynonyms: N,6,6-Trimethyl-N-(naphthalen-1-ylmethyl)hept-2-en-4-yn-1-amineCAS NO: 91161-71-6Molecular Formula: C21H25N.HClMolecular Weight: 327.90Purity: ≥99%Solubility: Storage: −20°C

prudect name : Terbinafine hydrochloride Synonyms: N,6,6-Trimethyl-N-(naphthalen-1-ylmethyl)hept-2-en-4-yn-1-amineCAS NO: 91161-71-6Molecular Formula: C21H25N.HClMolecular Weight: 327.90Purity: ≥99%Solubility: Storage: −20°C 2 years web site: www.medchemexpress.com

๐Ÿ“Œ
0๐Ÿ’ฌ read more

Torezolid phosphate is a novel oxazolidinone for gram-positive infections, has an IC50 of 8.7 _mu_M and 5.7 _mu_M for monoamine oxidase (MAO)-A and MAO-B, respectively.

prudect name : Torezolid phosphate is a novel oxazolidinone for gram-positive infections, has an IC50 of 8.7 _mu_M and 5.7 _mu_M for monoamine oxidase (MAO)-A and MAO-B, respectively.Tedizolid phosphate Synonyms:…

๐Ÿ“Œ
0๐Ÿ’ฌ read more

Trichostatin A (TSA) is a selective and potent HDAC inhibitor with IC50 of ~1.8 nM; HDAC8 is the only known member of the HDAC-family that is not affected by TSA.

prudect name : Trichostatin A (TSA) is a selective and potent HDAC inhibitor with IC50 of ~1.8 nM; HDAC8 is the only known member of the HDAC-family that is not…

๐Ÿ“Œ
0๐Ÿ’ฌ read more

prudect name : TorasemideSynonyms: CAS NO: 56211-40-6Molecular Formula: C16H20N4O3SMolecular Weight: 348.42Purity: ≥99%Solubility: Storage: -20°C

prudect name : Torasemide Synonyms: CAS NO: 56211-40-6Molecular Formula: C16H20N4O3SMolecular Weight: 348.42Purity: ≥99%Solubility: Storage: -20°C web site: www.medchemexpress.com

๐Ÿ“Œ
0๐Ÿ’ฌ read more

Tubastatin A is substantially selective for all 11 HDAC isoforms and maintains over 1000-fold selectivity against all isoforms excluding HDAC8, where it has approximately 57-fold selectivity. In homocysteic acid (HCA) induced neurodegeneration assays, Tubastatin A displays dose-dependent protection against HCA-induced neuronal cell death starting at 5 ยฆรŒM with near complete protection at 10 ยฆรŒM.

prudect name : Tubastatin A is substantially selective for all 11 HDAC isoforms and maintains over 1000-fold selectivity against all isoforms excluding HDAC8, where it has approximately 57-fold selectivity. In…

๐Ÿ“Œ
0๐Ÿ’ฌ read more

Torcetrapib dose-dependently increases aldosterone release from H295R cells after either 24 or 48 h of treatment with an EC50 of approximately 80 nM, this effect is mediated by calcium channel as calcium channel blockers completely blocks torcetrapib-induced corticoid release and calcium increase. Torcetrapib (1 ยฆรŒM) significantly increases the expression of steroidogenic gene, CYP11B2 and CYP11B1, in H295R cell lines.

prudect name : Torcetrapib dose-dependently increases aldosterone release from H295R cells after either 24 or 48 h of treatment with an EC50 of approximately 80 nM, this effect is mediated…

๐Ÿ“Œ
0๐Ÿ’ฌ read more