2. Cell Cycle/DNA Damage
    Apoptosis
  3. CDK
    Apoptosis
  4. SY-5609

SY-5609  (Synonyms: CDK7-IN-3)

Cat. No.: HY-138293 Purity: 99.66%
COA Handling Instructions

SY-5609 (CDK7-IN-3) is an orally active, highly selective, noncovalent CDK7 inhibitor with a KD of 0.065 nM. SY-5609 shows poor inhibition on CDK2 (Ki=2600 nM), CDK9 (Ki=960 nM), CDK12 (Ki=870 nM). SY-5609 induces apoptosis in tumor cells and has antitumor activity.

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

SY-5609 Chemical Structure

SY-5609 Chemical Structure

CAS No. : 2417302-07-7

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5 mg USD 550 In-stock
Estimated Time of Arrival: December 31
10 mg USD 900 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1800 In-stock
Estimated Time of Arrival: December 31
50 mg USD 3000 In-stock
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100 mg USD 4600 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

SY-5609 (CDK7-IN-3) is an orally active, highly selective, noncovalent CDK7 inhibitor with a KD of 0.065 nM. SY-5609 shows poor inhibition on CDK2 (Ki=2600 nM), CDK9 (Ki=960 nM), CDK12 (Ki=870 nM). SY-5609 induces apoptosis in tumor cells and has antitumor activity[1][2].

IC50 & Target[1]

CDK7

0.065 nM (Kd)

CDK2

2600 nM (Ki)

CDK9

960 nM (Ki)

CDK12

870 nM (Ki)

In Vitro

SY-5609 (0.01-10000 nM; 72 hours) demonstrates strong antiproliferative effects in triple negative breast cancer (TNBC) and ovarian (OVA) cancer cells[1].
SY-5609 (100-500 nM; 48, 72 hours) induces apoptosis[1].
SY-5609 (100-500 nM; 48 hours) induces G2/M cell cycle arrest in HCC70 cells[1].
SY-5609 (25-500 nM; 6-48 hours) results in inhibition of the phosphorylation of CDK2 at Thr160 via loss of CAK function for 24 and 48 h[1].
SY-5609 (compound 101; 126.4 pM-4 µM; 72 hours) has an EC50 of 5.6 nM in HCC70 cell line[2].

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

Cell Proliferation Assay[1]

Cell Line: HCC70, MDA-MB453, COV504, A2780, OVCAR3, CAOV3 cells
Concentration: 0.01-10000 nM
Incubation Time: 72 hours
Result: Demonstrated strong antiproliferative effects with IC50 of 1-6 nM.

Apoptosis Analysis[1]

Cell Line: HCC70, MDA-MB-468, CAOV3 and OVCAR3 cells
Concentration: 100, 250, 500 nM
Incubation Time: 48 and 72 hours
Result: Induced apoptosis.

Cell Cycle Analysis[1]

Cell Line: HCC70 cells
Concentration: 100, 250, 500 nM
Incubation Time: 48 hours
Result: Induced G2/M cell cycle arrest.

Western Blot Analysis[1]

Cell Line: HCC70 cells
Concentration: 25, 50, 100, 250, 500 nM
Incubation Time: 6, 24, 48 hours
Result: Resulted in inhibition of the phosphorylation of CDK2 at Thr160 via loss of CAK function for 24 and 48 h.
In Vivo

SY-5609 (2 mg/kg/day; orally; for 21 days) induces tumor regression over the 21-day dosing period[1].
Daily oral dosing of 2 mg/kg SY-5609 in mice provided a plasma exposure of 261.28 ng h/mL with a Cmax of 50.67 ng/mL (103 nM) and an elimination half-life of 3.33 h[1].

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

Animal Model: Six-to-eight-week-old Balb/c nude female mice with HCC70 cell line[1]
Dosage: 2 mg/kg
Administration: Orally; daily; for 21 days
Result: Induced tumor regression over the 21-day dosing period and was well tolerated. No regrowth of tumor was observed out to day 28.
Clinical Trial
Molecular Weight

490.46

Appearance

Solid

Formula

C23H26F3N6OP
CAS No.
SMILES

N#CC1=C(P(C)(C)=O)C2=C(C=C1)C(C3=NC(N[[email protected]@H]4CNC(C)(C)CC4)=NC=C3C(F)(F)F)=CN2
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 : 40 mg/mL (81.56 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0389 mL 10.1945 mL 20.3890 mL
5 mM 0.4078 mL 2.0389 mL 4.0778 mL
10 mM 0.2039 mL 1.0195 mL 2.0389 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 4 mg/mL (8.16 mM); Suspended solution; Need ultrasonic

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 4 mg/mL (8.16 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.5 mg/mL (5.10 mM); Clear solution

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

Purity: 99.66%

COA (263 KB) HNMR (256 KB) LCMS (110 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:

SY-56092417302-07-7CDK7-IN-3SY5609SY 5609CDKApoptosisCyclin dependent kinaseHCC70MDA-MB453COV504A2780OVCAR3CAOV3triplenegativebreastovarianG2/MCDK2Thr160Inhibitorinhibitorinhibit

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