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BSJ-03-204

Cat. No. M13398
BSJ-03-204  Structure
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Quality Control & Documentation
Biological Activity

BSJ-03-204 is a Cereblon ligand linked to THE CDK ligand PROTAC, which is an effective, selective cdK4/6 dual inhibitor based on Palbociclib. The IC50 of CDK4/D1 and CDK6/D1 were 26.9 nM and 10.4 nM, respectively.

Chemical Information
Molecular Weight 832.9
Formula C43H48N10O8
CAS Number 2349356-09-6
Solubility (25°C) DMSO ≥ 60 mg/mL
Storage -20°C, protect from light, dry, sealed
Conversion of different model animals based on BSA (PMID: 27057123)
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.

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DGY-09-192 is a bivalent degrader that couples the pan-FGFR inhibitor BGJ398 to the CRL2VHL E3 ligase-recruiting ligand, which induces degradation of FGFR1/2 and largely avoids degradation of FGFR3/4.DGY-09-192 exhibits a nanomolar DC50 against both wild-type FGFR2 and several FGFR2 fusions. In addition, DGY-09-192 has antiproliferative activity in gastric and cholangiocarcinoma cells.

BTX-6654

BTX-6654 is a targeted and specific cerebellar-based bifunctional SOS1 PROTAC degrader.BTX-6654 reduces the downstream signaling markers pERK and pS6 and displays antiproliferative activity in a wide range of KRAS-mutant cells.

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KT-294

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  Catalog
Abmole Inhibitor Catalog




Keywords: BSJ-03-204 supplier, PROTAC, inhibitors, activators


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