CJ-2360

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

CJ-2360 

CJ-2360 是一种有效的口服 ALK 抑制剂,对野生型 ALK 和 F1197M、G1269A、L1196M 和 S1206Y ALK 突变体的 IC50 分别为 2.2、4.0、8.8、6.3 和 8.9 nM。CJ-2360 对临床报道的两种 ALK 突变体 (C1156Y 和 L1196M) 以及 468 种激酶 (LTK、MERTK、CLK1、DAPK1 和 DAPK2) 具有较强的抑制活性。

CJ-2360

CJ-2360 Chemical Structure

CAS No. : 2226742-61-4

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生物活性

CJ-2360 is a potent and orally active ALK inhibitor with IC50s of 2.2, 4.0, 8.8, 6.3, and 8.9 nM against wild-type ALK and F1197M, G1269A, L1196M, and S1206Y ALK mutants, respectively. CJ-2360 displays potent inhibitory activity against two clinically reported ALK mutants (C1156Y and L1196M) and a few other kinases (LTK, MERTK, CLK1, DAPK1, and DAPK2) among the 468 kinases evaluated[1].

体外研究
(In Vitro)

CJ-2360 achieves an IC50 value of 1.8 nM in inhibition of cell growth in the KARPAS-299 cell line. Further tested CJ-2360 for its potency in cell growth inhibition in the H3122 non-small-cell lung cell line carrying EML4-ALK and obtained an IC50 value of 3 nM. CJ-2360 inhibits Mer tyrosine-protein kinase (MERTK), CLK1, DAPK1, DAPK2, and DAPK3 with IC50s of 6.3, 11, 31, 23, 22, and 260 nM, respectively. CJ-2360 displays >100-fold selectivity for ALK over the insulin receptor kinase (INSR) and shows no significant activity against IGF1R[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

CJ-2360 (100 mg/kg; p.o.; twice daily for 22 days) is capable of achieving complete and long-lasting tumor regression in the KARPAS-299 xenograft tumor model[1].
CJ-2360 (100 mg/kg; p.o.) is very effective in inhibition of ALK phosphorylation, as well as ERK and STAT3 phosphorylation in KARPAS-299 tumor tissue, with the effect persisting for at least 24 h[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: KARPAS-299 xenograft model (female SCID mice)[1]
Dosage: 100 mg/kg
Administration: P.o.; twice daily for 22 days
Result: Very efficacious in the KARPAS-299 xenograft model. It achieves complete tumor regression in 100% of tumors and all tumors did not return until day 53, 23 days after the last dose.

分子量

475.56

Formula

C27H30FN5O2

CAS 号

2226742-61-4

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.

参考文献
  • [1]. Chen J, et al. Discovery of CJ-2360 as a Potent and Orally Active Inhibitor of Anaplastic Lymphoma Kinase Capable of Achieving Complete Tumor Regression. J Med Chem. 2020;63(22):13994-14016.

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