Tamnorzatinib ONO-7475|cas:1646839-59-9|西域试剂

Tamnorzatinib ONO-7475,98.07%

产品编号：Bellancom-114358| CAS NO：1646839-59-9| 分子式：C₃₂H₂₆N₄O₆| 分子量：562.57

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货号	价格	库存与货期
Bellancom-114358	￥1550.00	杭州北京（现货）
Bellancom-114358	￥2400.00	杭州北京（现货）
Bellancom-114358	￥6000.00	杭州北京（现货）

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Tamnorzatinib ONO-7475

产品介绍

Tamnorzatinib (ONO-7475) 是一种有效的、选择性的、具有口服活性的 Axl/Mer 抑制剂，IC₅₀ 值分别为 0.7 nM 和 1.0 nM。Tamnorzatinib 使 AXL 过表达的 EGFR 突变型 NSCLC 细胞对 EGFR-TKIs 敏感，抑制耐药细胞的产生和耐药性的维持。Tamnorzatinib 联合 Osimertinib (HY-15772) 为 EGFR 突变非小细胞肺癌 (NSCLC) 的研究提供了一个光明的前景。

生物活性

Tamnorzatinib (ONO-7475) is a potent, selective, and orally active Axl/Mer inhibitor with IC₅₀ values of 0.7 nM and 1.0 nM, respectively. Tamnorzatinib sensitizes AXL-overexpressing EGFR-mutant NSCLC cells to the EGFR-TKIs, suppresses the emergence and maintenance of tolerant cells. Tamnorzatinib combines with Osimertinib (HY-15772) provides a bright promise for the study of?EGFR-mutated non-small cell lung cancer (NSCLC).

体外研究

Tamnorzatinib is against recombinant human AXL with IC₅₀ values of 0.414 nM and 0.7 nM in off-chip MSA and ACD cell-based tyrosine kinase assay, respectively. It is against AXL, MER, TYRO3, TRKB, PDGFR alpha, TRKA, and FLT3 activities with IC₅₀ values of 0.7 nM, 1.0 nM, 8.7 nM, 15.8 nM, 28.9 nM, 35.7 nM and 147 nM, respectively in a Cell-based Tyrosine Kinase assay.
Tamnorzatinib (0.0001 μM-1 μM; 72 hours) increases the sensitivity to Osimertinib and Dacomitinib and reduces the viability of high AXL-expressing PC-9 and HCC4011 cells, but not of low-AXL-expressing HCC827 cells. Besides, Tamnorzatinib enhances Osimertinib efficacy on the viability of cell lines PC-9, PC-9KGR, and HCC4011, and H1975, all of which express high levels of AXL. But it has a marginal effect on the viability of cell lines HCC827, HCC4006, and H3255 with low levels of AXL.
Tamnorzatinib (1 μM; 4 or 48 hours) combines with Osimertinib markedly inhibits the phosphorylation of AXL, AKT, and p70S6K compared with the treatment of the high-AXL-expressing cell lines treated with Osimertinib alone at 4 hours. It combines with osimertinib increases cleaved PARP in PC-9 and HCC4011 cells compared with the treatment with Osimertinib alone.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay

Cell Line:	High AXL-expressing cell: PC-9,HCC4011,H1975, PC-9KGR cells Low AXL-expressing cell: HCC827, HCC4006, and H3255 cells
Concentration:	0.0001 μM; 0.001 μM; 0.01 μM; 0.1 μM; 1 μM
Incubation Time:	72 hours
Result:	Increased the sensitivity and efficacy to Osimertinib in AXL-high level cells.

Western Blot Analysis

Cell Line:	PC-9, HCC4011 cells
Concentration:	1 μM
Incubation Time:	4 or 48 hours
Result:	Increased p-AXL, AKT, and p70S6K expression at 4 hours and increases p-PARP expression at 48 hours when combindes with Osimertinib.

体内研究
(In Vivo)

Tamnorzatinib (oral gavage; 10 mg/kg or combines with 5 mg/kg Osimertinib; 29 days) treatment alone has little effect on the tumor growth. Besides, Osimertinib alone causes tumor regression within one week, but the tumors reappear within three weeks. The combined initial treatment causes tumor regression and the size of tumors is maintained for 4 weeks. No apparent adverse events, including weight loss are observed during these treatments.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Mouse CDX model using high-AXL-expressing PC-9KGR cells (exon 19 deletion and the exon21-T790M mutation in EGFR)
Dosage:	10 mg/kg; once daily; 19 days
Administration:	oral gavage
Result:	Had little effects alone, but combined treatments significantly decreased tumor volume without reappear.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Mouse CDX model using high-AXL-expressing PC-9KGR cells (exon 19 deletion and the exon21-T790M mutation in EGFR)
Dosage:	10 mg/kg; once daily; 19 days
Administration:	oral gavage
Result:	Had little effects alone, but combined treatments significantly decreased tumor volume without reappear.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Mouse CDX model using high-AXL-expressing PC-9KGR cells (exon 19 deletion and the exon21-T790M mutation in EGFR)
Dosage:	10 mg/kg; once daily; 19 days
Administration:	oral gavage
Result:	Had little effects alone, but combined treatments significantly decreased tumor volume without reappear.

性状

Solid

溶解性数据

In Vitro:

DMSO : 250 mg/mL (444.39 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.7776 mL	8.8878 mL	17.7756 mL
5 mM	0.3555 mL	1.7776 mL	3.5551 mL
10 mM	0.1778 mL	0.8888 mL	1.7776 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。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式