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ChemicalBook--->CAS DataBase List--->2785430-90-0

2785430-90-0

2785430-90-0 Structure

2785430-90-0 Structure
IdentificationBack Directory
[Name]

2,4-Pyrimidinediamine, N4-(8-methyl-4-cinnolinyl)-N2-[3-(4-morpholinyl)phenyl]-
[CAS]

2785430-90-0
[Synonyms]

ALK5-IN-34
2,4-Pyrimidinediamine, N4-(8-methyl-4-cinnolinyl)-N2-[3-(4-morpholinyl)phenyl]-
[Molecular Formula]

C23H23N7O
[MOL File]

2785430-90-0.mol
[Molecular Weight]

413.48
Chemical PropertiesBack Directory
[Boiling point ]

688.9±65.0 °C(Predicted)
[density ]

1.341±0.06 g/cm3(Predicted)
[form ]

Solid
[pka]

5.12±0.40(Predicted)
[color ]

Light yellow to green yellow
Hazard InformationBack Directory
[Uses]

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].
[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.
[IC 50]

ALK5: <10 nM (IC50)
[References]

[1] Bettina FRANZ, et al. Alk-5 inhibitors and uses thereof. Patent. WO2022126133A1.
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