2. Cell Cycle/DNA Damage
    Apoptosis
  3. CDK
    Apoptosis
  4. CDKI-73

CDKI-73  (Synonyms: LS-007)

Cat. No.: HY-12445 Purity: 99.76%
COA Handling Instructions

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. CDKI-73 down-regulates the RNAPII phosphorylation. CDKI-73 is also a novel pharmacological inhibitor of Rab11 cargo delivery and innate immune secretion.

For research use only. We do not sell to patients.

CDKI-73 Chemical Structure

CDKI-73 Chemical Structure

CAS No. : 1421693-22-2

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 462 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 462 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 420 In-stock
Estimated Time of Arrival: December 31
10 mg USD 600 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1800 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2520 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 3 publication(s) in Google Scholar

Top Publications Citing Use of Products

    CDKI-73 purchased from MCE. Usage Cited in: Am J Cancer Res. 2020 Apr 1;10(4):1140-1155.   [Abstract]

    The expression of BRCA1, p-CDK9, CDK9, Bcl-2 proteins, γ-H2AX, cleaved PARP, and cleaved caspase-3 in HO8910 cells treated with CDKI-73.

    View All CDK Isoform Specific Products:

    View All Isoforms
    CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    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. CDKI-73 down-regulates the RNAPII phosphorylation. CDKI-73 is also a novel pharmacological inhibitor of Rab11 cargo delivery and innate immune secretion[1][2][3][4].
    IC50 & Target[6][1]

    CDK2

    3.27 nM (IC50)

    CDK9

    5.78 nM (IC50)

    CDK1

    8.17 nM (IC50)

    CDK4

    8.18 nM (IC50)

    CDK6

    37.68 nM (IC50)

    CDK7

    134.26 nM (IC50)

    CDK1

    4 nM (Ki)

    CDK2

    3 nM (Ki)

    CDK9

    4 nM (Ki)

    CDK7

    91 nM (Ki)

    In Vitro

    CDKI-73 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].
    CDKI-73 (0.1 μM, 4 h) inhibits the phosphorylation of serine 2 of RNA polymerase II and MCL1 protein expression in CLL cells[1].
    CDKI-73 induced caspase-dependent apoptosis that was preceded by dephosphorylation of cdk9 and serine 2 of RNA polymerase II[1].
    CDKI-73 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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Viability Assay[1].

    Cell Line: CLL cells.
    Concentration: 0-1 μM.
    Incubation Time: 48 h.
    Result: Shows preferential cytotoxicity in CLL cells.
    In Vivo

    CDKI-73 (25, 50, 100 mg/kg) markedly decreases tumor growth in a dose-dependent manner and results in a prolongation of animal life span (P < 0.001) without causing body weight loss and other overt toxicities.[3].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: MV4-11 tumor bearing mice[3].
    Dosage: 25 mg/kg.
    Administration: Orally once everyday for 33 days.
    Result: Caused a remarkable delay in tumor growth compared to vehicle-treated mice, as reflected in a percentage for the mean tumor volume in treated to control mice of 43% at day 31.
    Animal Model: Balb/C mice aged 6-8 weeks[3].
    Dosage: 2 mg/kg (IV), 10, 20 and 40 mg/kg (PO). (Pharmacokinetic Analysis.)
    Administration: IV and PO, single dose.
    Result: The Cmax increased from 1.29 to 3.66 μM at a mean time of 1 h and the area under the curve (AUC) of CDKI-73 increased from 3.51 to 12.8 μM.h when the oral dose was escalated from 10 to 40 mg/kg.
    CDKI-73 was eliminated from plasma with a mean terminal half-life (T1/2) of 2 h. Its oral bioavailability (F) ranged from 54 to 85% across the three doses.
    Molecular Weight

    394.45

    Appearance

    Solid

    Formula

    C15H15FN6O2S2
    CAS No.
    SMILES

    CNC1=NC(C)=C(C2=C(F)C=NC(NC3=CC(S(=O)(N)=O)=CC=C3)=N2)S1
    Shipping

    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)
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 52 mg/mL (131.83 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.5352 mL 12.6759 mL 25.3518 mL
    5 mM 0.5070 mL 2.5352 mL 5.0704 mL
    10 mM 0.2535 mL 1.2676 mL 2.5352 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.67 mg/mL (6.77 mM); Clear solution

    *All of the co-solvents are available by MCE.
    Purity & Documentation

    Purity: 99.76%

    COA (249 KB) LCMS (270 KB)

    Handling Instructions (2659 KB)
    References
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    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Keywords:

    CDKI-731421693-22-2LS-007CDKI73CDKI 73LS007LS 007CDKApoptosisCyclin dependent kinaseCLLleukemiaAcutemyeloidAMLlowtoxicityendosomeInhibitorinhibitorinhibit

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