详情描述
Taletrectinib (DS-6051b, AB-106) is a new-generation selective ROS1/NTRK inhibitor with ic50 of 0.207 nM, 0.622 nM, 2.28 nM and 0.980 nM for ROS1, NTRK1, NTRK2 and NTRK3, respectively.
Product information
CAS Number: 1505515-69-4
Molecular Weight: 551.61
Formula: C29H34FN5O5
Synonym:
DS-6051B adipate
Chemical Name: 3-[4-[((2R)-2-Aminopropyl)oxy]phenyl]-N-[(1R)-1-(3-fluorophenyl)ethyl]imidazo[1, 2-b]pyridazin-6-amine monoadipate
Smiles: C[C@@H](NC1C=CC2=NC=C(C3C=CC(=CC=3)OC[C@@H](C)N)N2N=1)C1=CC(F)=CC=C1.OC(=O)CCCCC(O)=O
InChiKey: DORJQZDOULKINH-QNBGGDODSA-N
InChi: InChI=1S/C23H24FN5O.C6H10O4/c1-15(25)14-30-20-8-6-17(7-9-20)21-13-26-23-11-10-22(28-29(21)23)27-16(2)18-4-3-5-19(24)12-18;7-5(8)3-1-2-4-6(9)10/h3-13,15-16H,14,25H2,1-2H3,(H,27,28);1-4H2,(H,7,8)(H,9,10)/t15-,16-;/m1./s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO: 50 mg/mL (90.64 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.
Shelf Life: ≥360 days 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:
DS-6051b inhibited the growth of the CD74-ROS1 overexpressed Ba/F3 cells and the ROS1 fusion-positive HCC78 cancer cell line.DS-6051b potently inhibited autophosphorylation of ROS1 in CD74-ROS1–expressed Ba/F3 cells and the SLC34A2-ROS1 harboring HCC78 cells at approximately single-digit to double-digit nanomolar concentration.
In Vivo:
In vivo experiments using the KM12-bearing mouse xenograft model shows that DS-6051b induced tumor shrinkage at a ≥50 mg/kg or higher treatment dose without significant body weight loss.
References:
- Katayama R,et al.Nat Commun. 2019 9;10(1):3604.
Products are for research use only. Not for human use.