2. Protein Tyrosine Kinase/RTK Apoptosis
  3. Anaplastic lymphoma kinase (ALK) Apoptosis
  4. ALK-IN-22

ALK-IN-22 (compound I-24) 是一种有效的 ALK 抑制剂，对于 ALK, ALKL1196M and ALKG1202R 的 IC50 值分别为 2.3、3.7 和 2.9 nM。ALK-IN-22 下调 ALK 及其下游蛋白的磷酸化。ALK-IN-22 诱导细胞凋亡 (apoptosis) 。ALK-IN-22 可用于肿瘤研究。

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ALK-IN-22 Chemical Structure

ALK-IN-22 Chemical Structure

CAS No. : 2468219-09-0

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ALK-IN-22 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-22 (compound I-24) is a potent ALK inhibitor with IC50 values of 2.3, 3.7 and 2.9 nM for ALK, ALKL1196M and ALKG1202R, respectively. ALK-IN-22 down-regulated the phosphorylation of ALK and its downstream proteins. ALK-IN-22 induces apoptosis. ALK-IN-22 can be used for tumor research[1].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
2.39 μM
Compound: I-24
Antiproliferative activity against EGFR positive human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against EGFR positive human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
[PMID: 35691173]
BaF3 IC50
> 1 μM
Compound: I-24
Antiproliferative activity IL3 dependent human Ba/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity IL3 dependent human Ba/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
[PMID: 35691173]
HCT-116 IC50
1.34 μM
Compound: I-24
Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
[PMID: 35691173]
HEK-293T IC50
> 10 μM
Compound: I-24
Antiproliferative activity against human HEK293T cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human HEK293T cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
[PMID: 35691173]
Hep 3B2 IC50
0.059 μM
Compound: I-24
Antiproliferative activity against human Hep3B cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human Hep3B cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
[PMID: 35691173]
HT-29 IC50
2.01 μM
Compound: I-24
Antiproliferative activity against human HT-29 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human HT-29 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
[PMID: 35691173]
KARPAS-299 IC50
0.011 μM
Compound: I-24
Antiproliferative activity against NPM-ALK positive human KARPAS-299 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against NPM-ALK positive human KARPAS-299 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
[PMID: 35691173]
MCF7 IC50
2.16 μM
Compound: I-24
Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
[PMID: 35691173]
MDA-MB-231 IC50
1.88 μM
Compound: I-24
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
[PMID: 35691173]
NCI-H1581 IC50
0.957 μM
Compound: I-24
Antiproliferative activity against human NC-H1581 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human NC-H1581 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
[PMID: 35691173]
NCI-H2228 IC50
0.037 μM
Compound: I-24
Antiproliferative activity against EML4-ALK positive human NCI-H2228 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against EML4-ALK positive human NCI-H2228 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
[PMID: 35691173]
NCI-H3122 IC50
0.027 μM
Compound: I-24
Antiproliferative activity against EML4-ALK positive human NC-H3122 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against EML4-ALK positive human NC-H3122 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
[PMID: 35691173]
PC-3 IC50
1.38 μM
Compound: I-24
Antiproliferative activity against human PC-3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human PC-3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
[PMID: 35691173]
体外研究
(In Vitro)

ALK-IN-22 (compound I-24) (72 hours) has anti-proliferative activities against ALK-positive karpas299, H2228 and H3122 cell lines with IC50 values of 11, 37 and 27 nM, respectively[1].
ALK-IN-22 (compound I-24) (0-100 nM; 24 hours; H2228 cells) has inhibitory effect on ALK and downstream signaling AKT and ERK[1].
ALK-IN-22 (compound I-24) (0-100 nM; 48 hours; H2228 cells) can induce apoptosis and achieve cell cycle arrest in G1 phase[1].

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

ALK-IN-22 相关抗体:

Western Blot Analysis[1]

Cell Line: H2228 cells
Concentration: 0, 25, 50 and 100 nM
Incubation Time: 24 hours
Result: Downregulated the phosphorylation level of ALK and blocked the expressions of ALK downstream key signaling AKT, ERK along with their activated forms in a dose-dependent fashion.

Apoptosis Analysis[1]

Cell Line: H2228 cells
Concentration: 0, 25, 50 and 100 nM
Incubation Time: 48 hours
Result: The apoptotic rates were 14.23%, 23.94% and 31.70% at concentrations of 25 nM, 50 nM and 100 nM, respectively.

Cell Cycle Analysis[1]

Cell Line: H2228 cells
Concentration: 0, 25, 50 and 100 nM
Incubation Time: 48 hours
Result: The percentage of cells in the G1 phase increased from 49.72% to 58.51% in a dose-dependent fashion.
体内研究
(In Vivo)

ALK-IN-22 (compound I-24) (25-50 mg/kg; i.g.; Twice daily, for 14 days) has antitumor efficacy in vivo[1].
ALK-IN-22 (compound I-24) (10 mg/kg; p.o.) shows the Cmax and t1/2 values of 345.7 ng/mL and 4.1 hours, respectively[1].
ALK-IN-22 (compound I-24) (2 mg/kg; i.v.) shows the CL and t1/2 values of 36.2 mL/min/kg and 2.5 hours, respectively[1].

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

Animal Model: Female BALB / c nude mice[1]
Dosage: 25 and 50 mg/kg
Administration: Intragastric; Twice daily, for 14 days.
Result: The tumor growth inhibition (TGI) value of 50 mg/kg reached 93.5%.
Animal Model: SD rats[1]
Dosage: 2 and 10 mg/kg (Pharmacokinetic Analysis)
Administration: Oral administration and intravenous injection
Result: 1.19
Parameter F16 VP-16
Dose (i.v.) mg/kg 10 10
Cmax (ng/mL) 26952 17712
Tmax (min) 5 5
AUCplasma (min*ng/mL) 2878363 409528
T1/2 (min) 151 45
Vd (L/Kg) 0.2341 0.432
CL (L/min/kg) 0.001 0.007
分子量

477.95

Formula

C24H24ClN7O2
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-22 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-222468219-09-0Anaplastic lymphoma kinase (ALK)ApoptosisAnaplastic lymphoma kinaseALK tyrosine kinase receptorCD246Cluster of differentiation 246apoptosisALKphosphorylationantitumorInhibitorinhibitorinhibit

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