1. Protein Tyrosine Kinase/RTK
  2. ALK
  3. ALK-IN-12

ALK-IN-12 

Cat. No.: HY-108230
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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.

For research use only. We do not sell to patients.

ALK-IN-12 Chemical Structure

ALK-IN-12 Chemical Structure

CAS No. : 1197958-53-4

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Description

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].

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.

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).
Molecular Weight

500.96

Formula

C₂₄H₃₀ClN₆O₂P

CAS No.
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ALK-IN-12
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HY-108230
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