| Stereochemistry | ACHIRAL |
| Molecular Formula | C23H28N8O |
| Molecular Weight | 432.5214 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CCN1C(=CC2=C1N=C(NC3=NN(C)C(C)=C3)C4=C2N(C)C=N4)C(=O)N(C5CC5)C6CC6
InChI
InChIKey=JCINBYQJBYJGDM-UHFFFAOYSA-N
InChI=1S/C23H28N8O/c1-5-30-17(23(32)31(14-6-7-14)15-8-9-15)11-16-20-19(24-12-28(20)3)21(26-22(16)30)25-18-10-13(2)29(4)27-18/h10-12,14-15H,5-9H2,1-4H3,(H,25,26,27)
| Molecular Formula | C23H28N8O |
| Molecular Weight | 432.5214 |
| Charge | 0 |
| Count |
MOL RATIO
1 MOL RATIO (average) |
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
BMS 911543 is a selective orally administered small molecule inhibitor of Janus kinase 2 (JAK2), developed by BristolMyers Squibb for the myelofibrosis treatment. BMS 911543 displayed potent antiproliferative effects in mutated JAK2expressing cell lines. A superior antiproliferative response occurred in primary progenitor cells isolated from patients with JAK2positive myeloproliferative disease (MPD) compared with those isolated from healthy volunteers. In vivo, a single oral dose of BMS 911543 resulted in durable JAK2phosphorylated STAT signalling pathway inhibition in multiple species. In a JAK2expressing xenograft model (SET2), BMS 911543 displayed a minimally effective dose of <2 mg/kg on phosphorylated STAT5 pathway inhibition.
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Approval Year
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The Brca1-KPC mice( 5–6 weeks of age, with a pancreatic mass of approximately 50–100 mm3) were treated for 2 weeks by daily oral gavage at a dose of 30 mg/kg BMS-911543. BMS-911543 treated mice had an overall reduction in bioluminescent imaging signal as compared to the vehicle controls
Route of Administration:
Oral
