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)- manufacturers
- SRX3207
-
- $51.00
-
2026-09-10
- CAS:2254693-15-5
- Purity: 99.85%
- Supply Ability: 10g
|
| | 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)- Basic information |
| | 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 |
| storage temp. | Store at -20°C | | solubility | DMSO : 5 mg/mL (9.00 mM; Need ultrasonic) | | form | Solid | | color | Light yellow to light brown |
| | 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)- Usage And Synthesis |
| 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 |
|