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  
Synthetic products have potential research and development risk.

* 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.

SHR5428 Related Classifications

  • 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

 

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

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