7H-Thieno[3,2-b]pyran-7-one, 3-[4-[[4-[4-(1-azetidinylmethyl)-3-methyl-1H-pyrazol-1-yl]-2-pyrimidinyl]amino]phenyl]-5-(4-morpholinyl)-
- Product Name
- 7H-Thieno[3,2-b]pyran-7-one, 3-[4-[[4-[4-(1-azetidinylmethyl)-3-methyl-1H-pyrazol-1-yl]-2-pyrimidinyl]amino]phenyl]-5-(4-morpholinyl)-
- CAS No.
- 2254693-15-5
- Chemical Name
- 7H-Thieno[3,2-b]pyran-7-one, 3-[4-[[4-[4-(1-azetidinylmethyl)-3-methyl-1H-pyrazol-1-yl]-2-pyrimidinyl]amino]phenyl]-5-(4-morpholinyl)-
- Synonyms
- SRX3207;SRX-3207,SRX3207;7H-Thieno[3,2-b]pyran-7-one, 3-[4-[[4-[4-(1-azetidinylmethyl)-3-methyl-1H-pyrazol-1-yl]-2-pyrimidinyl]amino]phenyl]-5-(4-morpholinyl)-
- CBNumber
- CB28095086
- Molecular Formula
- C29H29N7O3S
- Formula Weight
- 555.65
- MOL File
- 2254693-15-5.mol
7H-Thieno[3,2-b]pyran-7-one, 3-[4-[[4-[4-(1-azetidinylmethyl)-3-methyl-1H-pyrazol-1-yl]-2-pyrimidinyl]amino]phenyl]-5-(4-morpholinyl)- Property
- storage temp.
- Store at -20°C
- solubility
- DMSO : 5 mg/mL (9.00 mM; Need ultrasonic)
- form
- Solid
- color
- Light yellow to light brown
N-Bromosuccinimide Price
- Product number
- CS-0120685
- Product name
- SRX3207
- Purity
- 98.92%
- Packaging
- 5mg
- Price
- $400
- Updated
- 2021/12/16
- Product number
- CS-0120685
- Product name
- SRX3207
- Purity
- 98.92%
- Packaging
- 10mg
- Price
- $680
- Updated
- 2021/12/16
- Product number
- CS-0120685
- Product name
- SRX3207
- Purity
- 98.92%
- Packaging
- 25mg
- Price
- $1350
- Updated
- 2021/12/16
- Product number
- CS-0120685
- Product name
- SRX3207
- Purity
- 98.92%
- Packaging
- 50mg
- Price
- $2200
- Updated
- 2021/12/16
- Product number
- CS-0120685
- Product name
- SRX3207
- Purity
- 98.92%
- Packaging
- 100mg
- Price
- $3400
- Updated
- 2021/12/16
7H-Thieno[3,2-b]pyran-7-one, 3-[4-[[4-[4-(1-azetidinylmethyl)-3-methyl-1H-pyrazol-1-yl]-2-pyrimidinyl]amino]phenyl]-5-(4-morpholinyl)- Chemical Properties,Usage,Production
Uses
SRX3207 is an orally active and first-in-class dual Syk/PI3K inhibitor, with IC50 values of 10.7 nM and 861 nM for Syk and PI3Kα, respectively. SRX3207 relieves tumor immunosuppression[1][2].
Biological Activity
SRX3207 is an orally active and first-in-class dual Syk/PI3K inhibitor, with IC50 values of 10.7 nM and 861 nM for Syk and PI3Kα, respectively. SRX3207 relieves tumor immunosuppression[1][2]. SRX3207 (10 μmol/L) is able to block p-AKT at concentration[1].SRX3207 has sufficient solubility in water (43 μmol/L)[1]. SRX3207 (10 mg/kg, orally) increases antitumor immune response[1].
in vivo
SRX3207 (10 mg/kg, orally) increases antitumor immune response[1].
| Animal Model: | LLC or B16 or B16-OVA or CT26 (1 × 105) cells were injected subcutaneously into syngeneic mice[1]. |
| Dosage: | 10 mg/kg. |
| Administration: | Orally, starting from day 10 when tumors reached 100 mm3 until tumors were harvested on day 21. |
| Result: | Blocked phosphorylation of Syk at 348 site and Y525/526 site. Blocked immunosuppressive MΦ polarization. Blocked tumor growth and increased survival effectively. |
IC 50
Syk: 10.7 nM (IC50); PI3Kα: 861 nM (IC50); PI3Kδ: 1280 nM (IC50); PI3Kγ: 11100 nM (IC50); Zap70: 1300 nM (IC50)
References
[1]. Shweta Joshi, et al. Macrophage Syk-PI3Kγ Inhibits Antitumor Immunity: SRX3207, a Novel Dual Syk-PI3K Inhibitory Chemotype Relieves Tumor Immunosuppression. Molecular Cancer Therapeutics. 2020. [2]. Shweta Joshi, et al. Macrophage Syk-PI3Kγ Inhibits Antitumor Immunity: SRX3207, a Novel Dual Syk-PI3K Inhibitory Chemotype Relieves Tumor Immunosuppression. Mol Cancer Ther. 2020 Mar;19(3):755-764.
7H-Thieno[3,2-b]pyran-7-one, 3-[4-[[4-[4-(1-azetidinylmethyl)-3-methyl-1H-pyrazol-1-yl]-2-pyrimidinyl]amino]phenyl]-5-(4-morpholinyl)- Preparation Products And Raw materials
Raw materials
Preparation Products
7H-Thieno[3,2-b]pyran-7-one, 3-[4-[[4-[4-(1-azetidinylmethyl)-3-methyl-1H-pyrazol-1-yl]-2-pyrimidinyl]amino]phenyl]-5-(4-morpholinyl)- Suppliers
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