Cat. No.: HY-155787

SHR5428

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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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Pureté: 99.80%
CAS No.: 3054791-71-5
Formule: C₂₂H₂₃F₃N₅O₂P
Masse moléculaire:477.42

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

SHR5428 Chemical Structure

CAS No.: 3054791-71-5

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Activité biologique
- Description
- IC₅₀ & Target
- In Vivo
Chemical Information
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

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)

Voir tous les produits spécifiques à Isoform CDK :

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)
C_max (ng/mL)	116	120	543
AUC (ng/mL∗h)	139	556	4101
t_1/2 (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%).

Chemical Information

CAS No. 3054791-71-5
Appearance Solid
Masse moléculaire 477.42
Formule C₂₂H₂₃F₃N₅O₂P
Color White to light yellow
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
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvant et solubilité

In Vitro:

DMSO : 25 mg/mL (52.36 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.0946 mL

10.4730 mL

20.9459 mL

5 mM

0.4189 mL

2.0946 mL

4.1892 mL

10 mM

0.2095 mL

1.0473 mL

2.0946 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

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

Solubility: ≥ 2.5 mg/mL (5.24 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.24 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (277 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Jia M, et al. Discovery of SHR5428 as a selective and noncovalent inhibitor of CDK7. Bioorg Med Chem Lett. 2023 Sep 1;93:129429. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.0946 mL	10.4730 mL	20.9459 mL	52.3648 mL
	5 mM	0.4189 mL	2.0946 mL	4.1892 mL	10.4730 mL
	10 mM	0.2095 mL	1.0473 mL	2.0946 mL	5.2365 mL
	15 mM	0.1396 mL	0.6982 mL	1.3964 mL	3.4910 mL
	20 mM	0.1047 mL	0.5236 mL	1.0473 mL	2.6182 mL
	25 mM	0.0838 mL	0.4189 mL	0.8378 mL	2.0946 mL
	30 mM	0.0698 mL	0.3491 mL	0.6982 mL	1.7455 mL
	40 mM	0.0524 mL	0.2618 mL	0.5236 mL	1.3091 mL
	50 mM	0.0419 mL	0.2095 mL	0.4189 mL	1.0473 mL

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SHR5428

Voir tous les produits spécifiques à Isoform CDK

Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

SHR5428 Related Classifications

HY-155787 Related Classifications