JAK3-IN-13
JAK3-IN-13 (compound 12n) is a potent, selective and orally active JAK3 inhibitor with IC50 values of 4728, 2039, 8, 365 nM for NK1, JNK2, JNK3, Tyk2, respectively. JAK3-IN-13 shows antiproliferative activity. JAK3-IN-13 induces cell cycle arrest at G0/G1 phase. JAK3-IN-13 shows antitumor activity.
For research use only. We do not sell to patients.
- CAS No.: 2803329-86-2
- Formula: C25H33ClN6O5
- Molecular Weight:533.02
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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JNK1 4728 nM (IC50) |
JNK2 2039 nM (IC50) |
JNK3 8 nM (IC50) |
Tyk2 365 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BaF3 | IC50 |
134.2 nM
Compound: 12n
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Antiproliferative activity against mouse BaF3 cells harboring TEL-JAK2 fusion protein assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay
Antiproliferative activity against mouse BaF3 cells harboring TEL-JAK2 fusion protein assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay
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[PMID: 35860875] |
| BaF3 | IC50 |
165.1 nM
Compound: 12n
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Antiproliferative activity against mouse BaF3 parent cell measured after 72 hrs by CCK-8 assay
Antiproliferative activity against mouse BaF3 parent cell measured after 72 hrs by CCK-8 assay
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[PMID: 35860875] |
| BaF3 | IC50 |
177.7 nM
Compound: 12n
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Antiproliferative activity against mouse BaF3 cells harboring TEL-JAK1 fusion protein assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay
Antiproliferative activity against mouse BaF3 cells harboring TEL-JAK1 fusion protein assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay
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[PMID: 35860875] |
| BaF3 | IC50 |
22.9 nM
Compound: 12n
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Antiproliferative activity against mouse BaF3 cells harboring JAK3 M5111 mutant assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay
Antiproliferative activity against mouse BaF3 cells harboring JAK3 M5111 mutant assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay
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[PMID: 35860875] |
| U-937 | IC50 |
20.2 nM
Compound: 12n
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Antiproliferative activity against human U-937 cells harboring JAK3 M511135 mutant assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay
Antiproliferative activity against human U-937 cells harboring JAK3 M511135 mutant assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay
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[PMID: 35860875] |
JAK3-IN-13 (compound 12n) (10 μM; 72 h) shows antiproliferative activity in BaF3-JAK3M511I, U937, parental cells[1].
JAK3-IN-13 inhibits the activity of TEL-JNK1, TEL-JNK2, JNK3M511I, JNK3 with IC50 values of 177.7, 134.2, 22.9, 1.2 nM, respectively[1].
JAK3-IN-13 inhibits (0-800 nM; 0-24 h) decreases the expression of phosphorylation JAK3, STAT3, and STAT5 in a dose-dependent manner[1].
JAK3-IN-13 inhibits (0-330 nM; 24 h) induces cell cycle arrest at G0/G1 phase and down-regulates the expression of cyclin-dependent kinase 2 (CDK2), CDK4, CDK6, cyclin B1, cyclin D3, and cyclin E1 in a concentration-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:BaF3-JAK3M511I, U937, parental, COLO-205, H1299, HCT-116, MDA-MB-231, AGS, HL 7702 cells
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Concentration:10 μM
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Incubation Time:72 h
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Result:Showed antiproliferative activity with IC50s of 22.9, 20.2, 165.1 nM for BaF3-JAK3M511I, U937, parental cells, and >10, >10, >10, >10, >10, 3.27 μM for COLO-205, H1299, HCT-116, MDA-MB-231, AGS, HL 7702 cells, respectively.
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Cell Line:U937 cells
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Concentration:0-800 nM
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Incubation Time:0-24 h
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Result:Dose-dependently suppressed the phosphorylation of JAK3, STAT3, and STAT5 and achieved near-complete inhibition at 200 nM.
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Cell Line:U937 cells
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Concentration:0-330 nM
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Incubation Time:24 h
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Result:Induced cell cycle arrest at G0/G1 phase and down-regulated the expression of cyclin-dependent kinase 2 (CDK2), CDK4, CDK6, cyclin B1, cyclin D3, and cyclin E1 in a concentration-dependent manner.
JAK3-IN-13 (12.5, 25, 50 mg/kg; p.o.; twice daily for 10 days) shows antitumor activity and inhibits the expression of phosphorylation JAK3, STAT3, STAT5, CDK2, CDK4, CDK6, cyclin B1, cyclin D3, and cyclin E1[1]. Pharmacokinetic Parameters of JAK3-IN-13 in Male Sprague-Dawley rats[1].
| 12n | i.v.(5 mg/kg) | p.o.(15 mg/kg) |
| anminal no. | 3 | 3 |
| T1/2 (h) | 0.91 | 0.98 |
| Cmax (ng/mL) | 911.33 | 238.28 |
| AUC(0-∞) (h·ng/mL) | 536.99 | 333.50 |
| CL (mL/min/kg) | 155.22 | |
| F % | 20.66 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Sprague-Dawley rats[1]
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Dosage:5 mg/kg for i.v.; 15 mg/kg for p.o.
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Administration:I.v. or p.o.
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Result:Showed good PK properties and oral bioavailability of 20.66%.
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Animal Model:Male CB17-SCID mice (U937 mouse xenograft model)[1]
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Dosage:12.5, 25, 50 mg/kg
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Administration:P.o.; twice daily for 10 days (10 mg/kg; i.p.; once daily)
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Result:Dose-dependently inhibited the growth of the U937 tumor and significantly inhibited the expression of phosphorylation JAK3, STAT3, and STAT5 as well as the cell cycle-related proteins.
Chemical Information
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CAS No. 2803329-86-2
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Molecular Weight 533.02
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Formula C25H33ClN6O5
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SMILES
C=CC(NC1=CC(NC2=NC=C(Cl)C(O[C@H]3[C@](OC[C@H]4OC)([H])[C@]4([H])OC3)=N2)=CC=C1N(CCN(C)C)C)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
JAK3-IN-13 Related Classifications
HY-150688 Related Classifications
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