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.

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (PROTAC CDK12/13 Degrader-1 TFA) usually boasts enhanced water solubility and stability.

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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PROTAC CDK12/13 Degrader-1 Related Antibodies

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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
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

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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PROTAC CDK12/13 Degrader-1 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.

Keywords:

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

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