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BOC Sciences |
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| Product Name: | GSK143 | | Synonyms: | GSK143;2-[[(3R,4R)-3-aminooxan-4-yl]amino]-4-(4-methylanilino)pyrimidine-5-carboxamide;GSK143
(GSK-143;5-Pyrimidinecarboxamide, 2-[[(3R,4R)-3-aminotetrahydro-2H-pyran-4-yl]amino]-4-[(4-methylphenyl)amino]- | | CAS: | 1240390-27-5 | | MF: | C17H22N6O2 | | MW: | 342.4 | | EINECS: | | | Product Categories: | | | Mol File: | 1240390-27-5.mol |  |
| | GSK143 Chemical Properties |
| storage temp. | Store at -20°C | | solubility | Soluble in DMSO |
| | GSK143 Usage And Synthesis |
| Uses | GSK 143 has pharmacological activity which is used in treatment of retinoblastoma protein (Rb)-positive cancers using kinase or BCL-2 inhibitors in combination with CDK4/6 inhibitors. | | in vivo | GSK143 (0.1-10 mg/kg; orally; 1.5 hours) reduces inflammation and prevents recruitment of immune cells in the intestinal muscularis of 1 mg/kg[3].
GSK143 (3, 10, 30, 100 mg/kg; oral; 1 hour before ovalbumin challenge) reduces the cutaneous reverse passive Arthus reaction in a dose dependent manner by approximately 50% and 70% at 10 mg/kg and 30 mg/kg, respectively[2].
GSK143 (iv of 1 mg/kg; po of 3 mg/kg) has a T1/2 of 4.2 hours, low clearance (16 mL/min/kg), moderate bioavailability of 30% and a Vss of 4.1 L/kg in rats[1].
| Animal Model: | Wild type C57NL/BL6 mice, 10-12 weeks old[3] | | Dosage: | 0.1, 1, 3, 10 mg/kg | | Administration: | Orally; 1.5 hours before intestinal manipulation (IM) | | Result: | Reduced inflammation and prevented recruitment of immune cells in the intestinal muscularis.
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| Animal Model: | Male CD rats (175-200 g)[1] | | Dosage: | 1 mg/kg of iv; 3 mg/kg of po (Pharmacokinetic Analysis) | | Administration: | IV or PO | | Result: | Had a T1/2 of 4.2 hours, low clearance (16 mL/min/kg), moderate bioavailability of 30% and a Vss of 4.1 L/kg.
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| | GSK143 Preparation Products And Raw materials |
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