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Chemical Structure| 1421693-22-2 Chemical Structure| 1421693-22-2

Structure of Asnuciclib
CAS No.: 1421693-22-2

Chemical Structure| 1421693-22-2

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Asnuciclib (CDKI-73; LS-007) is an orally active, potent CDK9 inhibitor with Ki values of 4 nM, 4 nM, and 3 nM for CDK9, CDK1, and CDK2, respectively. CDKI-73 downregulates the phosphorylation of RNA polymerase II and also serves as a Rab11 inhibitor.

Synonyms: CDKI-73; LS-007; asnuciclib [INN]

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Product Details of Asnuciclib

CAS No. :1421693-22-2
Formula : C15H15FN6O2S2
M.W : 394.45
SMILES Code : CNC1=NC(C)=C(C2=C(F)C=NC(NC3=CC(S(=O)(N)=O)=CC=C3)=N2)S1
Synonyms :
CDKI-73; LS-007; asnuciclib [INN]
MDL No. :MFCD28386217

Safety of Asnuciclib

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319
Precautionary Statements:P501-P270-P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313-P301+P312+P330

Related Pathways of Asnuciclib

Hedgehog

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Drosophila fat body cells 50 nM, 500 nM, 1 µM 15 minutes to 30 minutes CDKI-73 treatment resulted in a significant increase in the size of Rab11 multivesicular endosomes and reduced the delivery of Rab11 vesicles to the plasma membrane PMC7072129
KM12 0.972 μM 24 hours To evaluate the anti-proliferative activity of CDKI-73 on KM12 cells, results showed that CDKI-73 significantly inhibited cell growth within 24 hours. PMC6763784
COLO 205 0.017 μM 24 hours To evaluate the anti-proliferative activity of CDKI-73 on COLO 205 cells, results showed that CDKI-73 significantly inhibited cell growth within 24 hours. PMC6763784
HCT 116 0.081 μM 24 hours To evaluate the anti-proliferative activity of CDKI-73 on HCT 116 cells, results showed that CDKI-73 significantly inhibited cell growth within 24 hours. PMC6763784
THP-1 macrophages 50 nM, 100 nM 4 hours CDKI-73 significantly reduced the secretion of IL-6 and TNFα in LPS-stimulated THP-1 macrophages PMC7072129
HT29 0.25 μM 48 hours To evaluate the apoptosis-inducing effect of CDKI-73 on HT29 cells, results showed that CDKI-73 induced apoptosis through mitochondrial membrane potential reduction. PMC6763784
MEL-XY3 10 µM PLX4032 5 weeks To study the effects of long-term PLX4032 treatment on BRAFV600E-mutated melanoma cell lines. The majority of melanoma cells died, but a proportion of cells remained viable and quiescent, presenting senescent cancer stem cell-like characteristics. PMC7170042
Jurkat 100–200 nM 72 hours To evaluate the anti-proliferative activity of LS-007 against acute leukemia cell lines, the results showed that LS-007 had significant cytotoxicity against these cell lines. PMC5099409
THP-1 100–200 nM 72 hours To evaluate the anti-proliferative activity of LS-007 against acute leukemia cell lines, the results showed that LS-007 had significant cytotoxicity against these cell lines. PMC5099409
HL-60 100–200 nM 72 hours To evaluate the anti-proliferative activity of LS-007 against acute leukemia cell lines, the results showed that LS-007 had significant cytotoxicity against these cell lines. PMC5099409
Molt-4 100–200 nM 72 hours To evaluate the anti-proliferative activity of LS-007 against acute leukemia cell lines, the results showed that LS-007 had significant cytotoxicity against these cell lines. PMC5099409
U937 100–200 nM 72 hours To evaluate the anti-proliferative activity of LS-007 against acute leukemia cell lines, the results showed that LS-007 had significant cytotoxicity against these cell lines. PMC5099409
CCRF-CEM 100–200 nM 72 hours To evaluate the anti-proliferative activity of LS-007 against acute leukemia cell lines, the results showed that LS-007 had significant cytotoxicity against these cell lines. PMC5099409

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Balb/c nude mice HCT 116 xenograft model Oral 100 mg/kg Once every 3 days for 19 days To evaluate the anti-tumor efficacy of CDKI-73 in the HCT 116 xenograft model, results showed that CDKI-73 significantly inhibited tumor growth without overt toxicity. PMC6763784

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.54mL

0.51mL

0.25mL

12.68mL

2.54mL

1.27mL

25.35mL

5.07mL

2.54mL

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