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Taletrectinib free base (Synonyms: DS-6051b free base; AB-106 free base)
Taletrectinib (DS-6051b) free base 是一种有效的口服活性下一代选择性 ROS1/NTRK 抑制剂。Taletrectinib free base 分别以0.207、0.622、2.28 和 0.98 nM 的 IC50 对重组 ROS1、NTRK1、NTRK2 和 NTRK3 有较强的抑制作用。Taletrectinib free base还抑制 ROS1 G2032R 和其他抗 Crizotinib 的 ROS1 突变体。
Taletrectinib free base Chemical Structure
CAS No. : 1505514-27-1
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是否有货 |
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| 100 mg |
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| 250 mg |
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询价 |
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| 500 mg |
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* Please select Quantity before adding items.
Taletrectinib free base 的其他形式现货产品:
Taletrectinib
| 生物活性 |
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].
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体外研究
(In Vitro) |
The IC50 of Taletrectinib free base (1-1000 nM; 72 hours) against Ba/F3-TPM3-NTRK1, Ba/F3-ETV6-NTRK1, -NTRK2, -NTRK3, or KM12 cells is ~3-20 nM[1].
Taletrectinib free base (0.001-1000 nM; 2 hours) dose dependently inhibited autophosphorylation of ROS1 in U-118-MG cells in vitro[1].
Taletrectinib (DS-6051b) free base potently inhibits autophosphorylation of ROS1 in JFCR-165, JFCR-168, and MGH193-1B cells[1].
Taletrectinib free base partially suppresses phospho-NTRK1 at 10 nM, and completely suppresses by 100 nM. Taletrectinib free base potently inhibits recombinant ROS1, NTRK1, and NTRK3 in sub-nanomolar concentration in an ATP-competitive manner. Taletrectinib free base almost completely inhibits ACK, ALK, DDR1, and LTK at 0.2 μM among 160 kinases in the presence of 1 mM ATP, but did not inhibit other 152 kinases strongly[1].
Taletrectinib free base effectively inhibits Crizotinib-resistant ROS1 secondary mutations, including G2032R solvent front mutation[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay[1]
| Cell Line: |
TPM3-NTRK1-induced Ba/F3 cells, KM12 cells |
| Concentration: |
1-1000 nM |
| Incubation Time: |
72 hours |
| Result: |
Inhibited TPM3-NTRK1-induced Ba/F3 cells and KM12 cells viability. |
Western Blot Analysis[1]
| Cell Line: |
U-118 MG cells (harboring FIG-ROS1 fusion gene) |
| Concentration: |
0.001-1000 nM |
| Incubation Time: |
2 hours |
| Result: |
Dose dependently inhibited autophosphorylation of ROS1 in U-118-MG cells. |
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体内研究
(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].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
| 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. |
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| Clinical Trial |
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis.
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| 参考文献 |
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[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.
[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.
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