| Bioactivity | Asnuciclib (CDKI-73; LS-007) is an orally active and highly efficacious CDK9 inhibitor, with Ki values of 4 nM, 4 nM and 3 nM for CDK9, CDK1 and CDK2, respectively. Asnuciclib down-regulates the RNAPII phosphorylation. Asnuciclib is also a novel pharmacological inhibitor of Rab11 cargo delivery and innate immune secretion[1][2][3][4]. |
| Invitro | Asnuciclib is highly cytotoxic to primary leukemia cells derived from CLL patients (mean LD50 = 0.08 μM) and shows>500-fold selectivity for primary leukemia cells over normal B-lymphocytes (LD50=40.5 μM)[1].Asnuciclib (0.1 μM, 4 h) inhibits the phosphorylation of serine 2 of RNA polymerase II and MCL1 protein expression in CLL cells[1].Asnuciclib induced caspase-dependent apoptosis that was preceded by dephosphorylation of cdk9 and serine 2 of RNA polymerase II[1].Asnuciclib is highly effective against all cell lines tested with an IC50 in the range of 0.012-0.517 μM; in particular three MLL-AML cell lines, namely MOLM13, MV4-11 and THP-1, were highly sensitive to CDKI-73 with IC50 values <0.062 μM[3]. Cell Viability Assay[1]. Cell Line: |
| Name | Asnuciclib |
| CAS | 1421693-22-2 |
| Formula | C15H15FN6O2S2 |
| Molar Mass | 394.45 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen) |
Asnuciclib
CAS: 1421693-22-2 F: C15H15FN6O2S2 W: 394.45
Asnuciclib (CDKI-73; LS-007) is an orally active and highly efficacious CDK9 inhibitor, with Ki values of 4 nM, 4 nM and
Data collection：peptidedb@qq.com
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