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Gdc-0077 (RG6114) is an effective, oral, selective PI3Kα inhibitor (IC50=0.038 nM). Gdc-0077 (RG6114) exerts its activity by binding to the ATP binding site of PI3K, thereby inhibiting phosphorylation of PIP2 to PIP3. Compared with wild-type PI3Kα, GDC-0077 (RG6114) showed higher selectivity against mutants.
| 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.
| Molecular Weight | 407.37 |
| Formula | C18H19F2N5O4 |
| CAS Number | 2060571-02-8 |
| Purity | >98% |
| Solubility | DMSO ≥ 60 mg/mL |
| Storage | at -20°C |
| Related PI3K Products |
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| Zandelisib
Zandelisib (ME-401) is a PI3K inhibitor that selectively inhibits P110 δ with an IC50 value of 3.5 nM. For details, please refer to compound 1 in patent literature WO2019183226 A1. Zandelisib has antitumor effects. |
| Quercetin (97%)
Quercetin is a PI3K inhibitor with IC50 of 2.4-5.4 μM that has been shown to cause potent reversible inhibition of fatty-acid synthase. |
| Erucic acid
Erucic acid is a monounsaturated fatty acid (MUFA) isolated from radish seeds. Erucic acid, which easily crosses the blood-brain barrier (BBB), normalizes the accumulation of long-chain fatty acids in the brain. |
| Linperlisib (YY-20394)
Linperlisib, also known as YY-20394 and PI3Kδ-IN-2, is a potent and selective PI3Kδ inhibitor. |
| Leniolisib
Leniolisib (CDZ173) is a potent and selective PI3Kδ inhibitor with IC50 of 11 nM. |
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