2. Protein Tyrosine Kinase/RTK
  3. Anaplastic lymphoma kinase (ALK)
  4. ALK-IN-12

ALK-IN-12 是一种有效且具有口服活性的 ALK 抑制剂，IC50 为 0.18 nM。ALK-IN-12 还抑制 IGF1R 和 InsR (IC50=20.3 和 90.6 nM)。具有抗肿瘤活性。

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ALK-IN-12 Chemical Structure

ALK-IN-12 Chemical Structure

CAS No. : 1197958-53-4

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ALK-IN-12 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

ALK-IN-12 is a potent and orally active ALK inhibitor with an IC50 of 0.18 nM. ALK-IN-12 also inhibits IGF1R and InsR (IC50=20.3 and 90.6 nM). Antitumor activities[1].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
KARPAS-299 IC50
28.3 nM
Compound: 11e
Antiproliferative activity against human ALK-positive KARPAS299 cells assessed as reduction in cell viability measured after 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
Antiproliferative activity against human ALK-positive KARPAS299 cells assessed as reduction in cell viability measured after 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
[PMID: 27144831]
U-937 IC50
1590 nM
Compound: 11e
Antiproliferative activity against human ALK-negative U937 cells assessed as reduction in cell viability measured after 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
Antiproliferative activity against human ALK-negative U937 cells assessed as reduction in cell viability measured after 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
[PMID: 27144831]
体外研究
(In Vitro)

ALK-IN-12 (compound 11e) effectively inhibits viability of the Karpas-299 ALCL cell line with an IC50 of 28.3 nM[1].

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

ALK-IN-12 相关抗体:
体内研究
(In Vivo)

ALK-IN-12 (10-50 mg/kg; orally; once daily for 13 consecutive days) shows dose-dependent antitumor activity[1].
ALK-IN-12 (3 mg/kg; i.v.; 6-8 week old female CD rats ) treatment shows AUC0-∞, CL, t1/2 and Vss are 3039 ng•h/mL, 0.91 h•kg, 6.6 hours and 6.12 L/kg, respectively[1].
ALK-IN-12 (10 mg/kg; p.o.; 6-8 week old female CD rats) treatment shows Cmax, AUC0-∞, tmax, t1/2 and F are 3254 ng/mL, 4056 ng•h/mL, 6.0 hours, 12.5 hours and 39%, respectively[1].

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

Animal Model: Eight- to 10-week old female SCID/beige mice (Karpas-299 xenograft mouse model expressing the NPM-ALK fusion)[1]
Dosage: 10-50 mg/kg
Administration: Orally; once daily for 13 consecutive days
Result: Dose-dependent antitumor activity. Led to tumor stasis (50 mg/kg dose).
分子量

500.96

Formula

C24H30ClN6O2P
CAS 号
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.
纯度 & 产品资料
参考文献

ALK-IN-12 相关分类

  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

ALK-IN-121197958-53-4Anaplastic lymphoma kinase (ALK)Anaplastic lymphoma kinaseALK tyrosine kinase receptorCD246Cluster of differentiation 246NSCLCmutationsresistanceKarpas-299ALCLcellInhibitorinhibitorinhibit

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