2. PROTAC Cell Cycle/DNA Damage
  3. PROTACs CDK
  4. PROTAC CDK12/13 Degrader-1 TFA

PROTAC CDK12/13 Degrader-1 TFA 

Cat. No.: HY-151110A Purity: 98.37%
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PROTAC CDK12/13 Degrader-1 (7f) TFA is a highly selective cell cycle protein-dependent kinase CDK12/CDK13 dual degrader with the DC50 values of 2.2 nM and 2.1 nM, respectively. PROTAC CDK12/13 Degrader-1 TFA has anti-proliferative activity and can be used in breast cancer research.

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

PROTAC CDK12/13 Degrader-1 TFA Chemical Structure

PROTAC CDK12/13 Degrader-1 TFA Chemical Structure

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1 mg USD 350 In-stock
5 mg USD 850 In-stock
10 mg USD 1350 In-stock
25 mg USD 2650 In-stock
50 mg USD 4100 In-stock
100 mg USD 6400 In-stock
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Based on 1 publication(s) in Google Scholar

Other Forms of PROTAC CDK12/13 Degrader-1 TFA:

PROTAC CDK12/13 Degrader-1 TFA Related Antibodies

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Description

PROTAC CDK12/13 Degrader-1 (7f) TFA is a highly selective cell cycle protein-dependent kinase CDK12/CDK13 dual degrader with the DC50 values of 2.2 nM and 2.1 nM, respectively. PROTAC CDK12/13 Degrader-1 TFA has anti-proliferative activity and can be used in breast cancer research[1].

IC50 & Target[1]

CDK12

2.2 nM (DC50)

CDK13

2.1 nM (DC50)

In Vitro

PROTAC CDK12/13 Degrader-1 (7f) TFA (0.02-10 μM, 150 h) significantly inhibits the proliferation of MFM223 and MDA-MB-231 cells in a dose-dependent manner[1].
PROTAC CDK12/13 Degrader-1 (7f) TFA (500 nM, 4 h) can significantly degrade CDK12 and CDK13 of MFM223 and MDA-MB-231 cells in a dose-dependent manner[1].

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

PROTAC CDK12/13 Degrader-1 TFA Related Antibodies

Immunofluorescence[1]

Cell Line: MDA-MB-231 cell lines
Concentration: 1.0 μM
Incubation Time: 15 hours
Result: Showed 88% degradation for CDK12 and 74% for CDK13.
Acted on CDK12 with the DC50 value of 2.2 nM, and acted on CDK13 with the DC50 value of 2.1 nM.
In Vivo

The pharmacokinetic parameters of PROTAC CDK12/13 Degrader-1 (7f) TFA in rats[1].

Parameters oral (20 mg/kg) iv (10 mg/kg) ip (20 mg/kg) iv (2.5 mg/kg)
t1/2 (h) - 5.28 10.85 5.8
Tmax (h) 5.33 0.08 2.17 0.08
Cmax (ng/mL) 7.73 19892.4 24.79 1498.5
Cmax (ng/mL) 7.73 19892.4 24.79 1498.5
AUC0-t(h*ng/mL) 21.83 7193.3 284.8 383.9
AUC0-∞(h*ng/mL) - 7242.7 318.5 391.55
CL (mL/h/kg) - 1406.5 - 6495.4
F (%) 0.15 - 10.63 -

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

936.93

Formula

C47H47F3N10O8
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(NCC1=CC=CC=C1)N([C@H]2CC[C@H](NC3=NC=C(C#N)C=C3)CC2)C4=CC=C(N5CCN(C(CNC6=CC7=C(C(N(C(CC8)C(NC8=O)=O)C7=O)=O)C=C6)=O)CC5)C=C4.O=C(O)C(F)(F)F
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (26.68 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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.0673 mL 5.3366 mL 10.6732 mL
5 mM 0.2135 mL 1.0673 mL 2.1346 mL
View the Complete Stock Solution Preparation Table

* 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 (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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C2

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V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* 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 (sealed storage, away from moisture and light). 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 1.0673 mL 5.3366 mL 10.6732 mL 26.6829 mL
5 mM 0.2135 mL 1.0673 mL 2.1346 mL 5.3366 mL
10 mM 0.1067 mL 0.5337 mL 1.0673 mL 2.6683 mL
15 mM 0.0712 mL 0.3558 mL 0.7115 mL 1.7789 mL
20 mM 0.0534 mL 0.2668 mL 0.5337 mL 1.3341 mL
25 mM 0.0427 mL 0.2135 mL 0.4269 mL 1.0673 mL
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PROTAC CDK12/13 Degrader-1 TFA Related Classifications

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:

PROTAC CDK12/13 Degrader-1PROTACsCDKCyclin dependent kinaseCDK12CDK13PROTACanti-proliferativebreast cancerTNBCInhibitorinhibitorinhibit

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