DS-6051
- CAS No.
- 1505514-27-1
- Chemical Name:
- DS-6051
- Synonyms
- DS-6051;DS-6051B;AB-106freebase;DS-6051b free base;Taletrectinib free base;N-Desmethyl N-Nitroso Tamoxifen-D3;Taletrectinib free base, 10 mM in DMSO;AB-106freebase|||Taletrectinib free base|||IBI-344 free base|||DS-6051b free base;Imidazo[1,2-b]pyridazin-6-amine, 3-[4-[(2R)-2-aminopropoxy]phenyl]-N-[(1R)-1-(3-fluorophenyl)ethyl]-
- CBNumber:
- CB44918275
- Molecular Formula:
- C23H24FN5O
- Molecular Weight:
- 405.47
- MDL Number:
- MFCD32708526
- MOL File:
- 1505514-27-1.mol
| Density | 1.27±0.1 g/cm3(Predicted) |
|---|---|
| pka | 8.37±0.10(Predicted) |
| FDA UNII | W4141180YD |
DS-6051 Chemical Properties,Uses,Production
Description
DS-6051b (Daiichi Sankyo, Japan) is an oral small molecule tyrosine kinase inhibitor that has demonstrated preclinical activity against ROS1 and NTRK1-3 rearrangements.
Uses
Taletrectinib (DS-6051b) free base is a potent, orally active, and next-generation selective ROS1/NTRK inhibitor. Taletrectinib free base potently inhibits recombinant ROS1, NTRK1, NTRK2, and NTRK3 with IC50s of 0.207, 0.622, 2.28, and 0.98 nM, respectively. Taletrectinib free base also inhibits ROS1 G2032R and other Crizotinib-resistant ROS1 mutants[1][2].
in vivo
Taletrectinib (DS-6051b) free base (25-200 mg/kg; p.o.; once daily for 18 days) shows antitumor activity[1].
Taletrectinib free base (6.25-200?mg/kg; p.o.; once daily for 8 days) inhibits NTRK-rearranged cancer in Balb-c nu/nu mice bearing KM12 cells[1].
Taletrectinib free base (3-100 mg/kg; p.o.; once daily for 4 days) shows rapid tumor regression in the wild-type (WT) and the G2032R-mutant Ba/F3-bearing mice without severe body weight loss[1].
| Animal Model: | Balb-c nu/nu mice (bearing U-118 MG cells)[1] |
| Dosage: | 25, 50, 100, and 200?mg/kg |
| Administration: | P.o.; once daily for 18 days |
| Result: | Effectively inhibited tumor growth at ≥25?mg/kg without significant body weight loss. |
References
[1] Katayama R, et al. The new-generation selective ROS1/NTRK inhibitor DS-6051b overcomes crizotinib resistant ROS1-G2032R mutation in preclinical models. Nat Commun. 2019;10(1):3604. Published 2019 Aug 9. DOI:10.1038/s41467-019-11496-z
[2] Fujiwara Y, et al. Safety and pharmacokinetics of DS-6051b in Japanese patients with non-small cell lung cancer harboring ROS1 fusions: a phase I study. Oncotarget. 2018;9(34):23729-23737. Published 2018 May 4. DOI:10.18632/oncotarget.25263
DS-6051 Preparation Products And Raw materials
Raw materials
Preparation Products
DS-6051 Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| Jinan Carbotang Biotech Co.,Ltd. | +8615866703830 | figo.gao@foxmail.com | China | 8497 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354; +17819995354 | marketing@targetmol.com | United States | 32435 | 58 |
| Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 | sales@sarms4muscle.com | China | 10473 | 58 |
| Zibo Hangyu Biotechnology Development Co., Ltd | +86-0533-2185556 +8615965530500 | nickzhang@hangyubiotech.com | China | 8510 | 58 |
| ChengDu TongChuangYuan Pharmaceutical Co.Ltd | 028-83379370 13880556291 | tcy@tcypharm.com | China | 7218 | 58 |
| Chuzhou KeMail Chemical Technology Co., Ltd | 0550-5196001 15000891977 | wj520wjxby@126.com | China | 1944 | 55 |
| Kaixin Chemical (Hong Kong) Limited | 010-88886666-01 13112345678 | loyson@tcypharm.com | China | 597 | 55 |
| Jinan Kabotang Biological Technology Co.,Ltd. | 0531-61320525 15866703830 | figo.gao@foxmail.com | China | 5177 | 58 |
| Chengdu dashengge pharmaceutical technology co., LTD | 13880556291 | fuwei@tcypharm.com | China | 235 | 58 |
| Jinan shenlikang chemical technology co. LTD | 0531-86092839 13153040268 | 2425815073@qq.com | China | 265 | 58 |
View Lastest Price from DS-6051 manufacturers
| Image | Update time | Product | Price | Min. Order | Purity | Supply Ability | Manufacturer | |
|---|---|---|---|---|---|---|---|---|
 |
2025-12-05 | Taletrectinib free base
1505514-27-1
|
US $65.00-255.00 / mg | 99.98% | 10g | TargetMol Chemicals Inc. |
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- Taletrectinib free base
1505514-27-1
- US $65.00-255.00 / mg
- 99.98%
- TargetMol Chemicals Inc.
