CDKI-73 (LS-007) is a potent CDK inhibitor with IC50 values of 8.17 nM, 3.27 nM, 8.18 nM and 5.78 nM for CDK1, CDK2, CDK4 and CDK9, respectively. CDKI-73 can induce apoptosis of cancer cells. CDKI-73 is an oral bioavailable and highly potent CDK9 inhibitor for the treatment of acute myeloid leukemia.

 

Brand: BCM

 

Target: CDK1:8.17 nM, CDK7:134.26 nM, CDK4:8.18 nM, CDK9:5.78 nM, CDK2:3.27 nM, CDK6:37.68 nM

 

Signaling Pathways: Apoptosis; Cell Cycle/Checkpoint

 

In Vivo: CDKI-73 exhibited a favorable pharmacokinetic profile with oral bioavailability of F = 56% following a single intravenous bolus dose at 2 mg/kg and an oral dose at 10 mg/kg in mice.

 

Boiling Point: 642.9±65.0 °C(Predicted)

 

pKa: 10.06±0.60(Predicted)

 

Solubility: Soluble in DMSO; soluble in Ethanol. Insoluble in Water.

 

Isomeric SMILES: CC1=C(SC(=N1)NC)C2=NC(=NC=C2F)NC3=CC(=CC=C3)S(=O)(=O)N  

 

InChIKey: GAIOPWBQKZMUNO-UHFFFAOYSA-N  

 

InChI: InChI=1S/C15H15FN6O2S2/c1-8-13(25-15(18-2)20-8)12-11(16)7-19-14(22-12)21-9-4-3-5-10(6-9)26(17,23)24/h3-7H,1-2H3,(H,18,20)(H2,17,23,24)(H,19,21,22)

 

Attribute
[Chem Name]	3-[[5-fluoro-4-[4-methyl-2-(methylamino)-1,3-thiazol-5-yl]pyrimidin-2-yl]amino]benzenesulfonamide
[Synonym]	CDKI-73; CDKI73; Asnuciclib; LS-007
[CAS No.]	1421693-22-2
[MDL No.]	MFCD28386217
[Formula]	C15H15FN6O2S2
[Molecular]	394.45
[Form]	Solid powder
[Storage]	Store at -20°C

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