2785430-90-0
2785430-90-0 structure
- Name: ALK5-IN-34
- Chemical Name: ALK5-IN-34
- CAS Number: 2785430-90-0
- Molecular Formula: C23H23N7O
- Molecular Weight: 413.48
- Catalog: Signaling Pathways Stem Cell/Wnt TGF-beta/Smad
- Create Date: 2022-10-08 09:15:50
- Modify Date: 2024-01-16 19:47:07
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ALK5-IN-34 is an selective orally active activin receptor-like kinase (ALK) inhibitor. ALK5-IN-34 can inhibit the activity of ALK5-IN-34 with an IC50 value of ≤10 nM. ALK5-IN-34 also has inhibitory of tumor growth and can be used for the research of proliferative diseases, such as cancer[1].
| Name | ALK5-IN-34 |
|---|
| Description | ALK5-IN-34 is an selective orally active activin receptor-like kinase (ALK) inhibitor. ALK5-IN-34 can inhibit the activity of ALK5-IN-34 with an IC50 value of ≤10 nM. ALK5-IN-34 also has inhibitory of tumor growth and can be used for the research of proliferative diseases, such as cancer[1]. |
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| Related Catalog | |
| Target |
ALK5:<10 nM (IC50) |
| In Vitro | ALK5-IN-34 (EX-11) has kinase inhibition of ALK5 with an IC50 value of ≤10 nM[1]. ALK5-IN-34 has kinase selectivity of ALK2/ALK5 with an IC50 value of ＜100 nM[1]. ALK5-IN-34 shows TGFB-RI inhibition (RD-SMAD receptor activity) with an IC50 value of ≤100 nM[1]. ALK5-IN-34 (1 μM-10 nM) inhibits the expression of TGF-β-mediated alpha-SMA in a full concentration-dependent[1]. ALK5-IN-34 (30, 300 and 3000 nM) suppresses the Treg frequency in a dose dependent manner[1]. ALK5-IN-34 (0-0.1 μM; for 6 days or 7 days) inhibits FOXL2CI34W-driven growth in KGN and COV434 cells with IC50 values of 140 nM and﹥10 μM, respectively[1]. ALK5-IN-34 (10, 100 and 1000 nM; 2 h) shows a dose-dependent decrease in pSmad2 in KGN cell line[1]. ALK5-IN-34 (30, 300 nM; 24 h) reverses the upregulation of gene expression in dose dependentent[1]. ALK5-IN-34 (30, 300 nM; 24 h) increases HLA class I expression in dose-dependent[1]. Cell Viability Assay[1] Cell Line: KGN and COV434 cell lines Concentration: 0-0.1 μM Incubation Time: for 6 days or 7 days Result: Inhibited FOXL2 CI34W -driven growth. RT-PCR[1] Cell Line: Human primary dermal fibroblasts Concentration: 30, 300 nM Incubation Time: 24 h Result: Reversed the upregulation of gene expression with TGFB stimulation. |
| In Vivo | ALK5-IN-34 (EX-11) (oral; 10-100 mg/kg) reduces the phopho SMAD2 levels (p-SMAD2) in a dose dependent manner in A549 murine xenograft model[1]. ALK5-IN-34 (oral; 75 mg/kg; 0-24 h) shows reversely correlated between PK and tumor PD (pSMAD2 levels)[1]. ALK5-IN-34 (oral; 150 mg/kg; bid; for 22 days) increases overall survival in ES-2 ovarian cancer mouse xenograft model and can delay progression[1]. ALK5-IN-34 (p.o.; 75, 150 mg/kg; twice a day; for 21days) shows tumor growth inhibition (TGI) and increases the survival when combining with anti-PD-L1/anti-PD-1 in Syngeneic TNBC Model and in Subcutaneous Cloudman S91 melanoma model[1]. ALK5-IN-34 (oral; 300, 1000 mg/kg; bid for 5 days) has good tolerability and safety margin in Tolerability Model[1]. Animal Model: A549 murine xenograft model[1] Dosage: 10, 50, 75 and 100 mg/kg Administration: oral gavage Result: Exhibited 92.5% inhibition based upon the average p-SMAD2 levels (75 mg/kg). Animal Model: EMT6 Syngeneic TNBC Model[1] Dosage: 75, 150 mg/kg Administration: p.o., twice a day, for 21days Result: Resulted significantly tumor growth inhibition (TGI) by 37% at 150 mg/kg. Result in significant tumor growth inhibition (TGI) with combination of anti-PD-LI and resulted in a significant increase in mean survival by 37%. Resulted in significant TGI by 34% with combination of anti-PD-1 and resulted in significant increase in mean survival by 26%. Decreased the intra-tumoral pressure. Animal Model: Cachexia Model[1] Dosage: 150 mg/kg Administration: oral gavage, twice a day for 22 days Result: Showed reduction in total fluid volume and high whole limb weights. |
| References |
[1]. Bettina FRANZ, et al. Alk-5 inhibitors and uses thereof. Patent. WO2022126133A1. |
| Molecular Formula | C23H23N7O |
|---|---|
| Molecular Weight | 413.48 |