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Taletrectinib free base
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Taletrectinib free base图片
CAS NO:1505514-27-1
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
DS-6051b free base
AB-106 free base
产品介绍
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。
生物活性

Taletrectinib (DS-6051b) free base is a potent, orally active, and next-generation selectiveROS1/NTRKinhibitor. Taletrectinib free base potently inhibits recombinant ROS1, NTRK1, NTRK2, and NTRK3 withIC50s 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].

体外研究
(In Vitro)

The IC50of 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].

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.
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].

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.
Clinical Trial
分子量

405.47

Formula

C23H24FN5O

CAS 号

1505514-27-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.