2. Cell Cycle/DNA Damage
  3. CDK
  4. 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).

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SHR5428 Chemical Structure

SHR5428 Chemical Structure

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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
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SHR5428 Related Classifications

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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.

Keywords:

SHR5428SHR 5428SHR-5428CDKCyclin dependent kinaseMDA-MB-468orally activeInhibitorinhibitorinhibit

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