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

PROTAC CDK12/13 Degrader-1 (7f) 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 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 Chemical Structure

PROTAC CDK12/13 Degrader-1 Chemical Structure

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1 mg USD 350 In-stock
5 mg USD 850 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

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PROTAC CDK12/13 Degrader-1 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

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Description

PROTAC CDK12/13 Degrader-1 (7f) 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 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) (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) (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 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) 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

822.91

Formula

C45H46N10O6
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 110 mg/mL (133.67 mM; Need ultrasonic; 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 1.2152 mL 6.0760 mL 12.1520 mL
5 mM 0.2430 mL 1.2152 mL 2.4304 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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
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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

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

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 (protect from 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 1.2152 mL 6.0760 mL 12.1520 mL 30.3800 mL
5 mM 0.2430 mL 1.2152 mL 2.4304 mL 6.0760 mL
10 mM 0.1215 mL 0.6076 mL 1.2152 mL 3.0380 mL
15 mM 0.0810 mL 0.4051 mL 0.8101 mL 2.0253 mL
20 mM 0.0608 mL 0.3038 mL 0.6076 mL 1.5190 mL
25 mM 0.0486 mL 0.2430 mL 0.4861 mL 1.2152 mL
30 mM 0.0405 mL 0.2025 mL 0.4051 mL 1.0127 mL
40 mM 0.0304 mL 0.1519 mL 0.3038 mL 0.7595 mL
50 mM 0.0243 mL 0.1215 mL 0.2430 mL 0.6076 mL
60 mM 0.0203 mL 0.1013 mL 0.2025 mL 0.5063 mL
80 mM 0.0152 mL 0.0759 mL 0.1519 mL 0.3797 mL
100 mM 0.0122 mL 0.0608 mL 0.1215 mL 0.3038 mL
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PROTAC CDK12/13 Degrader-1 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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