Product Name :
OTX015 — BET Inhibitor
Description:
OTX015 is a novel, highly potent, selective and cell permeable inhibitor of the bromodomain and extra terminal (BET) family proteins BRD2, BRD3 and BRD4 with IC50 of 10-19 nM. It inhibits the growth of a variety of human cancer cell lines with IC50 ranging from 60 to 200 nM. OTX015 results in rapid down-regulation of c-MYC expression, and show the synergistic anti-proliferative effects in combination with ALK inhibitors in ALKpos ALCL cell lines. In vivo studies using OTX015 have demonstrated efficacy in a range of oncology models. OTX015 is currently in phase I clinical development for oncology indication.
CAS:
202590-98-5
Molecular Weight:
491.99
Formula:
C25H22ClN5O2S
Chemical Name:
(S)-2-(4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)-N-(4-hydroxyphenyl)acetamide
Smiles :
CC1=NN=C2[C@H](CC(=O)NC3C=CC(O)=CC=3)N=C(C3=C(SC(C)=C3C)N12)C1C=CC(Cl)=CC=1
InChiKey:
GNMUEVRJHCWKTO-FQEVSTJZSA-N
InChi :
InChI=1S/C25H22ClN5O2S/c1-13-14(2)34-25-22(13)23(16-4-6-17(26)7-5-16)28-20(24-30-29-15(3)31(24)25)12-21(33)27-18-8-10-19(32)11-9-18/h4-11,20,32H,12H2,1-3H3,(H,27,33)/t20-/m0/s1
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.{{Thioridazine} site|{Thioridazine} Neuronal Signaling|{Thioridazine} Purity & Documentation|{Thioridazine} In Vitro|{Thioridazine} custom synthesis|{Thioridazine} Autophagy}
Shelf Life:
≥12 months if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.
Additional information:
OTX015 is a novel, highly potent, selective and cell permeable inhibitor of the bromodomain and extra terminal (BET) family proteins BRD2, BRD3 and BRD4 with IC50 of 10-19 nM. It inhibits the growth of a variety of human cancer cell lines with IC50 ranging from 60 to 200 nM. OTX015 results in rapid down-regulation of c-MYC expression, and show the synergistic anti-proliferative effects in combination with ALK inhibitors in ALKpos ALCL cell lines. In vivo studies using OTX015 have demonstrated efficacy in a range of oncology models. OTX015 is currently in phase I clinical development for oncology indication.|Product information|CAS Number: 202590-98-5|Molecular Weight: 491.99|Formula: C25H22ClN5O2S|Synonym:|Birabresib|MK-8628|Chemical Name: (S)-2-(4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)-N-(4-hydroxyphenyl)acetamide|Smiles: CC1=NN=C2[C@H](CC(=O)NC3C=CC(O)=CC=3)N=C(C3=C(SC(C)=C3C)N12)C1C=CC(Cl)=CC=1|InChiKey: GNMUEVRJHCWKTO-FQEVSTJZSA-N|InChi: InChI=1S/C25H22ClN5O2S/c1-13-14(2)34-25-22(13)23(16-4-6-17(26)7-5-16)28-20(24-30-29-15(3)31(24)25)12-21(33)27-18-8-10-19(32)11-9-18/h4-11,20,32H,12H2,1-3H3,(H,27,33)/t20-/m0/s1|Technical Data|Appearance: Solid Power.{{Cefepime} MedChemExpress|{Cefepime} Penicillin-binding protein (PBP)|{Cefepime} Protocol|{Cefepime} In stock|{Cefepime} custom synthesis|{Cefepime} Cancer} |Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: DMSO up to 100 mM|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.PMID:35227773 |Shelf Life: ≥12 months if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined.|HS Tariff Code: 382200|How to use|In Vitro:|OTX015 was used at 2-10 µM final concentration in various in vitro assays.|In Vivo:|OTX015 could be dosed to the mice by oral administration at 100 mg/kg once per day or 10 mg/kg twice per day.|References:|Noel JK, et al. Development of the BET bromodomain inhibitor OTX015. (2013) Mol Cancer Ther. 12, C244.Boi M, et al. OTX015, a bromodomain and extraterminal inhibitor, represents a novel agent for ALK positive anaplastic large cell lymphoma. (2013) Mol Cancer Ther. 12, A219.Products are for research use only. Not for human use.|Documents||
