Roginolisib (MSC2360844) hemifumarate is a potent, orally active and selective PI3Kδ inhibitor, with an IC50 of 145 nM. Roginolisib hemifumarate shows highly selective against a panel of 278 additional kinases.
Molecular Weight | 584.62 |
Formula | C26H27FN4O5S.1/2C4H4O4 |
CAS Number | 1621688-31-0 |
Form | Solid |
Solubility (25°C) | DMSO 100 mg/mL (ultrasonic) |
Storage | 4°C, dry, sealed |
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.
[3] M Gahr, et al. Pharmacopsychiatry. Aseptic gingivitis related to quetiapine hemifumarate
[5] K Kappert, et al. Dtsch Med Wochenschr. [Aliskiren hemifumarate]
Related PI3K Products |
---|
SNV4818
SNV4818 is a potential best-in-class (best-in-class) mutation-selective PI3K-α inhibitor with excellent selectivity for the H1047X mutant and moderate selectivity for the related E545/542X mutant. |
hSMG-1 inhibitor 11j
hSMG-1 inhibitor 11j, a pyrimidine derivative, is a potent and selective inhibitor of hSMG-1, with an IC50 of 0.11 nM. |
RLY-2608
RLY-2608 is a first-in-class, orally active, selective inhibitor of PI3Ka metabolism. |
EDI048
EDI048 is an orally active Cryptosporidium PI4K inhibitor for the research of cryptosporidiosis. |
PI3Kδ-IN-13
PI3Kδ-IN-13 is a PI3Kδ inhibitor (IC50=2.6 nM). |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.