BPR1K871 is a potent and selective dual FLT3/AURKA inhibitor with IC50s of 19 nM and 22 nM for FLT3 and AURKA, respectively, acts as a preclinical development candidate for anti-cancer therapy.
| Molecular Weight | 526.05 |
| Formula | C25H28ClN7O2S |
| CAS Number | 2443767-35-7 |
| Form | Solid |
| Solubility (25°C) | DMSO 125 mg/mL (ultrasonic) |
| 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 FLT3 Products |
|---|
| FLT3-IN-19
FLT3-IN-19 is a potent and selective FLT3 inhibitor with IC50 of 0.213 nM. |
| LT-540-717
LT-540-717 is a potent FLT3 inhibitor (IC50=0.62 nM) with antiproliferative activity. |
| GTP-14564
GTP-14564 is a tyrosine kinase inhibitor targeting to internal tandem duplication (ITD) and FLT3. |
| HDAC-IN-63
HDAC-IN-63 is a dual FLT3/HDAC inhibitor (IC50: 0.844 and 30.0 nM for FLT3 and HDAC1 respectively). |
| FLT3-IN-20
FLT3-IN-20 is a potent FLT3 inhibitor with IC50 values of 1 and 4 nM for FLT3-D835Y and FLT3-ITD, respectively. |
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