2. Cell Cycle/DNA Damage PROTAC Apoptosis
  3. CDK PROTACs Apoptosis
  4. YJ1206

YJ1206 is an orally active, selective CDK12/CDK13 PROTAC degrader with an IC50 of 12.55 nM for in VCaP cells. YJ1206 increases DNA damage, induces apoptosis, and promotes tumor regression in orthotopic WA74 patient-derived xenograft (PDX) mice models of resistant prostate cancer. YJ1206 suppresses tumor growth in vivo in conjunction with AKT pathway inhibitors. YJ1206 is composed of the CDK12/CDK13 degradation agent (HY-168658), a linker (HY-W004328), and a VHL E3 ubiquitin ligase (HY-W453548). (Pink: Navitoclax; Blue: VHL ligand; Black: linker).

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YJ1206 Chemical Structure

YJ1206 Chemical Structure

CAS No. : 3053716-98-3

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Based on 1 publication(s) in Google Scholar

YJ1206 Related Antibodies

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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Description

YJ1206 is an orally active, selective CDK12/CDK13 PROTAC degrader with an IC50 of 12.55 nM for in VCaP cells. YJ1206 increases DNA damage, induces apoptosis, and promotes tumor regression in orthotopic WA74 patient-derived xenograft (PDX) mice models of resistant prostate cancer. YJ1206 suppresses tumor growth in vivo in conjunction with AKT pathway inhibitors. YJ1206 is composed of the CDK12/CDK13 degradation agent (HY-168658), a linker (HY-W004328), and a VHL E3 ubiquitin ligase (HY-W453548). (Pink: Navitoclax; Blue: VHL ligand; Black: linker)[1].

IC50 & Target[1]

CDK12

 

CDK13

 

Molecular Weight

894.01

Formula

C49H52FN11O5
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(NCC1=CC=CC=C1)N(C2=CN=C(N3CCN(C4CCN(C5=C(F)C=C(C(N(C6CCC(NC6=O)=O)C7=O)=O)C7=C5)CC4)CC3)C=C2)[C@H](CC8)CC[C@@H]8NC9=NC=C%10C(C=CC=C%10)=N9
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 66.67 mg/mL (74.57 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 1.1186 mL 5.5928 mL 11.1856 mL
5 mM 0.2237 mL 1.1186 mL 2.2371 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. 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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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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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. 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 1.1186 mL 5.5928 mL 11.1856 mL 27.9639 mL
5 mM 0.2237 mL 1.1186 mL 2.2371 mL 5.5928 mL
10 mM 0.1119 mL 0.5593 mL 1.1186 mL 2.7964 mL
15 mM 0.0746 mL 0.3729 mL 0.7457 mL 1.8643 mL
20 mM 0.0559 mL 0.2796 mL 0.5593 mL 1.3982 mL
25 mM 0.0447 mL 0.2237 mL 0.4474 mL 1.1186 mL
30 mM 0.0373 mL 0.1864 mL 0.3729 mL 0.9321 mL
40 mM 0.0280 mL 0.1398 mL 0.2796 mL 0.6991 mL
50 mM 0.0224 mL 0.1119 mL 0.2237 mL 0.5593 mL
60 mM 0.0186 mL 0.0932 mL 0.1864 mL 0.4661 mL
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YJ1206 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:

YJ12063053716-98-3YJ 1206YJ-1206CDKPROTACsApoptosisCyclin dependent kinaseOrallyDNA damageorthotopicWA74PDXprostate cancerInhibitorinhibitorinhibit

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