1. Cell Cycle/DNA Damage
  2. CDK
  3. SHR5428

SHR5428 is a potent, orally active, selective and noncovalent inhibitor of CDK7 with highly potent CDK7 enzymatic activity (IC50=2.3 nM). SHR5428 inhibits triple negative breast cancer cellular activity on MDA-MB-468 cell (IC50=6.6 nM).

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

SHR5428 Chemical Structure

SHR5428 Chemical Structure

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

SHR5428 is a potent, orally active, selective and noncovalent inhibitor of CDK7 with highly potent CDK7 enzymatic activity (IC50=2.3 nM). SHR5428 inhibits triple negative breast cancer cellular activity on MDA-MB-468 cell (IC50=6.6 nM)[1].

IC50 & Target

CDK7

0.005 μM (IC50)

CDK12

1.11 μM (IC50)

CDK4

3.87 μM (IC50)

CDK6

5.89 μM (IC50)

CDK9

8.30 μM (IC50)

CDK2

8.99 μM (IC50)

CDK1

>100 μM (IC50)

In Vivo

SHR5428 (3-30 mg/kg, PO, once a day for 21 days) shows dose-dependent tumor growth inhibition[1].
SHR5428 (2 mg/kg, PO, once) displays favorable pharmacokinetic properties in different species such as mouse, rat and dog[1].
Pharmacokinetic Parameters of SHR5428 in mouse, rat and dog[1].

Mouse (2 mg/kg) Rat (2 mg/kg) Dog (2 mg/kg)
Cmax (ng/mL) 116 120 543
AUC (ng/mL∗h) 139 556 4101
t1/2 (h) 0.7 2.6 4.9
Bioavailability F% 32% 44%
92%

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

Animal Model: HCC70 cell line derived xenograft NDG mouse model[1]
Dosage: 3, 10, 30 mg/kg
Administration: PO, once a day for 21 days
Result: Showed dose-dependent tumor growth inhibition (3 mg/kg, TGI = 39%; 10 mg/kg, TGI = 61%; 30 mg/kg, TGI = 83%).
Molecular Weight

477.42

Formula

C22H23F3N5O2P

SMILES

CP(C1=C(C=CC2=C1NC=C2C3=C(C=NC(N[C@@H]4C[C@H](CCC4)O)=N3)C(F)(F)F)C#N)(C)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
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.

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
SHR5428
Cat. No.:
HY-155787
Quantity:
MCE Japan Authorized Agent: