Taletrectinib - CAS:1505515-69-4

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Taletrectinib (Synonyms:DS-6051b; AB-106)

目录号 : KM10611 CAS No. : 1505515-69-4 纯度 : 98%

Data Sheet 产品使用指南

Taletrectinib (DS-6051b) 是一种有效的口服活性下一代选择性 ROS1/NTRK 抑制剂。Taletrectinib 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 还抑制 ROS1 G2032R 和其他抗 Crizotinib 的 ROS1 突变体。

规格	价格	是否有货
5mg		In-stock
10mg		In-stock
50mg	询价	In-stock
100mg	询价	In-stock

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生物活性

Taletrectinib (DS-6051b) is a potent, orally active, and next-generation selective ROS1/NTRK inhibitor. Taletrectinib potently inhibits recombinant ROS1, NTRK1, NTRK2, and NTRK3 with IC₅₀s of 0.207, 0.622, 2.28, and 0.98 nM, respectively. Taletrectinib also inhibits ROS1 G2032R and other Crizotinib-resistant ROS1 mutants.

体外研究

The IC₅₀ of Taletrectinib (1-1000 nM; 72 hours) against Ba/F3-TPM3-NTRK1, Ba/F3-ETV6-NTRK1, -NTRK2, -NTRK3, or KM12 cells is ~3-20 nM.
Taletrectinib (0.001-1000 nM; 2 hours) dose dependently inhibited autophosphorylation of ROS1 in U-118-MG cells in vitro.
Taletrectinib potently inhibits autophosphorylation of ROS1 in JFCR-165, JFCR-168, and MGH193-1B cells.
Taletrectinib 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 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.
Taletrectinib effectively inhibits Crizotinib-resistant ROS1 secondary mutations, including G2032R solvent front mutation.

Cell Viability Assay

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

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

Taletrectinib (DS-6051b) (25-200 mg/kg; p.o.; once daily for 18 days) shows antitumor activity.
Taletrectinib (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.
Taletrectinib (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.

Animal Model:	Balb-c nu/nu mice (bearing U-118 MG cells)
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.

分子式

C₂₉H₃₄FN₅O₅

分子量

551.61

CAS号

1505515-69-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 50 mg/mL (90.64 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.8129 mL	9.0644 mL	18.1287 mL
5 mM	0.3626 mL	1.8129 mL	3.6258 mL
10 mM	0.1813 mL	0.9064 mL	1.8129 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (3.77 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.77 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (3.77 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.77 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (3.77 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.77 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

临床试验

纯度： 98%

Data Sheet

产品使用指南

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