LY-294,002 hydrochloride is a potent broad-spectrum PI3K inhibitor with IC50s of 0.5, 0.57, and 0.97 μM for P110α, P110δ, and P110β, respectively; in addition, LY294002 hydrochloride also inhibits CK2, with an IC50 of 98 nM, and can be used in studies related to pancreatic cancer. LY294002 hydrochloride can also inhibit CK2 with an IC50 of 98 nM.
| Molecular Weight | 343.8 |
| Formula | C19H17NO3 · HCl |
| CAS Number | 934389-88-5 |
| Solubility (25°C) | DMSO: ≥5 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 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). |
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