MSC-1186 is a highly selective pan-SRPK inhibitor with activity against SRPK1, SRPK2, and SRPK3 with IC50 values of 2.7 nM, 81 nM, and 0.6 nM, respectively.MSC-1186 can be used in cancer research.
| Molecular Weight | 461.90 |
| Formula | C19H17ClFN7O2S |
| CAS Number | 2871698-23-4 |
| Form | Solid |
| Solubility (25°C) | DMSO >100 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related SRPK Products |
|---|
| SRPKIN-1
SRPKIN-1 is a covalent and irreversible SRPK1/2 inhibitor with IC50s of 35.6 and 98 nM, respectively. Anti-angiogenesis effect. |
| WAY-652848
WAY-652848 is a selective inhibitor of SRPK1 with an IC50 value of 0.58 μM.WAY-652848 effectively reduces choroidal neovascularization (CNV) in vivo, and can be used in the study of age-related macular degeneration. |
| SPHINX31
SPHINX31 is a potent inhibitor of serine/arginine-rich protein kinase 1 (SRPK1) with IC50 of 5.9 nM. SPHINX31 inhibits phosphorylation of serine/arginine-rich splicing factor 1 (SRSF1). |
| SRPIN340
SRPIN340 is a selective SRPK inhibitor with Ki of 0.89 μM for SRPK1, showing no significant inhibitory activity against more than 140 other kinases. |
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