Information Taletrectinib (DS-6051b, AB-106) is a new-generation selectiveROS1/NTRKinhibitor with ic50 of 0.207 nM,0.622 nM,2.28 nM and 0.980 nM for ROS1,NTRK1,NTRK2 and NTRK3,respectively. Targets ROS1 (Cell-free assay); TrkA (Cell-free assay); TrkC (Cell-free assay); TrkB (Cell-free assay) 0.207 nM; 0.622 nM; 0.980 nM; 2.28 nM 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\u2009mg/kg or higher treatment dose without significant body weight loss.
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Taletrectinib
Dangerous GoodsCAS number:1505515-69-4 molecular formula:C29H34FN5O5
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Specs
| Chinese alias | 塔雷替尼 | ||
| English alias | Taletrectinib adipate | DS-6051b | HY-131003 | AB-106 | 3-[4-[((2R)-2-Aminopropyl)oxy]phenyl]-N-[(1R)-1-(3-fluorophenyl)ethyl]imidazo[1,2-b]pyridazin-6-amine monoadipate | DS-6051B adipate | Taletrectinib adipate [USAN] | AKOS040745032 | GLXC-25968 | 3-(4 | ||
| CAS number | 1505515-69-4 | molecular formula | C29H34FN5O5 |
| molecular weight | 551.61 g/mol | Exact mass | ≥99% |
| PSA | 152.000 Ų | logp | 2.17 |
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Safety information
pictogram:
GHS07
Signal word:
Warning
Hazard Statement:
H315: 引起皮肤刺激 H319: 引起严重眼睛刺激 H335: 可能引起呼吸道刺激 H302: 吞食有害
Statement of Preventive Measures:
P261: 避免吸入灰尘/烟雾/气体/雾/蒸汽/喷雾 P305+P351+P338: 如进入眼睛:用水小心冲洗几分钟。如戴隐形眼镜并可方便地取出,取出隐形眼镜。继续冲洗。 P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。 P302+P352: 如皮肤沾染:用水充分清洗。 P301+P312: 如误吞咽:如感觉不适,呼叫急救中心/医生。
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