ChemicalBook > CAS DataBase List > 4-Pyrimidinamine, N-[[4-(1-methyl-1H-pyrazol-4-yl)phenyl]methyl]-6-[7-[3-(1-pyrrolidinyl)propoxy]imidazo[1,2-a]pyridin-3-yl]-
4-Pyrimidinamine, N-[[4-(1-methyl-1H-pyrazol-4-yl)phenyl]methyl]-6-[7-[3-(1-pyrrolidinyl)propoxy]imidazo[1,2-a]pyridin-3-yl]-
- Product Name
- 4-Pyrimidinamine, N-[[4-(1-methyl-1H-pyrazol-4-yl)phenyl]methyl]-6-[7-[3-(1-pyrrolidinyl)propoxy]imidazo[1,2-a]pyridin-3-yl]-
- CAS No.
- 2590556-80-0
- Chemical Name
- 4-Pyrimidinamine, N-[[4-(1-methyl-1H-pyrazol-4-yl)phenyl]methyl]-6-[7-[3-(1-pyrrolidinyl)propoxy]imidazo[1,2-a]pyridin-3-yl]-
- Synonyms
- M4205;Velzatinib;M4205(IDRX-42);M4205, 10 mM in DMSO;factor,M-4205,receptor,M4205,cell,CD117,growth,inhibit,mast/stem,mutations,SCFR,c-Kit,M 4205,Inhibitor;N-(4-(1-Methyl-1H-pyrazol-4-yl)benzyl)-6-(7-(3-(pyrrolidin-1-yl)propoxy)imidazo[1,2-a]pyridin-3-yl)pyrimidin-4-amine;N-[[4-(1-Methylpyrazol-4-yl)phenyl]methyl]-6-[7-(3-pyrrolidin-1-ylpropoxy)imidazo[1,2-a]pyridin-3-yl]pyrimidin-4-amine;N-[[4-(1-Methyl-1H-pyrazol-4-yl)phenyl]methyl]-6-[7-[3-(1-pyrrolidinyl)propoxy]imidazo[1,2-a]pyridin-3-yl]-4-pyrimidinamine;4-Pyrimidinamine, N-[[4-(1-methyl-1H-pyrazol-4-yl)phenyl]methyl]-6-[7-[3-(1-pyrrolidinyl)propoxy]imidazo[1,2-a]pyridin-3-yl]-
- CBNumber
- CB68988841
- Molecular Formula
- C29H32N8O
- Formula Weight
- 508.62
- MOL File
- 2590556-80-0.mol
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4-Pyrimidinamine, N-[[4-(1-methyl-1H-pyrazol-4-yl)phenyl]methyl]-6-[7-[3-(1-pyrrolidinyl)propoxy]imidazo[1,2-a]pyridin-3-yl]- Property
- Density
- 1.30±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO : 11.11 mg/mL (21.84 mM; ultrasonic and warming and heat to 66°C)
- pka
- 10.01±0.20(Predicted)
- form
- Solid
- color
- White to light brown
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4-Pyrimidinamine, N-[[4-(1-methyl-1H-pyrazol-4-yl)phenyl]methyl]-6-[7-[3-(1-pyrrolidinyl)propoxy]imidazo[1,2-a]pyridin-3-yl]- Chemical Properties,Usage,Production
Uses
M4205 is a multi-target inhibitor for PDGFRB, PDGFRA, CSF1R, c-Kit, FLT3, and LCK, with an IC50s of 2.6, 50, 5.5, 44, 141 and 141 nM, respectively. M4205 exhibits antitumor efficacy in xenograft mouse models[1].
in vivo
M4205 (35 mg/kg for 30 days) exhibits antitumor efficacy in xenograft mouse models[1].
| Animal Model: | GIST430/654 xenograft models[1]. |
| Dosage: | 35 mg/kg |
| Administration: | 30 days |
| Result: | Inhibited tumor growth. |
IC 50
PDGFRβ: 2.6 nM (IC50); CSF1R: 5.5 nM (IC50); KIT: 44 nM (IC50); PDGFRA: 50 nM (IC50); Lck: 141 nM (IC50); FLT3: 141 nM (IC50)
References
[1] Blum A, et al. Identification of M4205─ A highly selective inhibitor of KIT mutations for treatment of unresectable metastatic or recurrent gastrointestinal stromal tumors[J]. Journal of Medicinal Chemistry, 2023, 66(4): 2386-2395.
4-Pyrimidinamine, N-[[4-(1-methyl-1H-pyrazol-4-yl)phenyl]methyl]-6-[7-[3-(1-pyrrolidinyl)propoxy]imidazo[1,2-a]pyridin-3-yl]- Preparation Products And Raw materials
Raw materials
Preparation Products
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4-Pyrimidinamine, N-[[4-(1-methyl-1H-pyrazol-4-yl)phenyl]methyl]-6-[7-[3-(1-pyrrolidinyl)propoxy]imidazo[1,2-a]pyridin-3-yl]- Suppliers
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