PROTAC CDK4/6/9 degrader 1 prodrug
PROTAC CDK4/6/9 degrader 1 prodrug is an orally active CDK4/CDK6/CDK9 PROTAC degrader prodrug. PROTAC CDK4/6/9 degrader 1 prodrug converts into PROTAC CDK4/6/9 degrader 1 (HY-178452). PROTAC CDK4/6/9 degrader 1 degrades CDK4, CDK6 and CDK9. PROTAC CDK4/6/9 degrader 1 prodrug is applicable to the research of triple-negative breast cancer (prodrug modification moiety: Lauric acid (HY-Y0366); PROTAC moiety: PROTAC CDK4/6/9 degrader 1 (HY-178452)).
For research use only. We do not sell to patients.
- Formula: C64H86N12O9
- Molecular Weight:1167.44
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Description
IC50 & Target
[1]|
CDK4 |
CDK6 |
CDK9 |
Cereblon |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK-293T | IC50 |
>15 μM
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Cytotoxicity against normal human HEK-293T cells assessed by cell viability assay.
Cytotoxicity against normal human HEK-293T cells assessed by cell viability assay.
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40977512 |
In Vitro
PROTAC CDK4/6/9 degrader 1 prodrug (Compound P4) is non-cytotoxic to normal LO2 and HEK-293T cells, with an IC50 >15 μM[1].
PROTAC CDK4/6/9 degrader 1 prodrug does not inhibit hERG protein, showing no potential cardiotoxicity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
| Species | Dose | Route | Bioavailability |
|---|---|---|---|
| Rat[1] | 30 mg/kg | p.o. | 35.3 % |
In Vivo
PROTAC CDK4/6/9 degrader 1 prodrug (30 mg/kg; p.o.; daily) potently inhibits TNBC lung metastasis in mice[1].
PROTAC CDK4/6/9 degrader 1 prodrug (30 mg/kg; p.o.; daily; 7 days) effectively inhibits tumor growth in TNBC mini-PDX models with favorable tolerability[1].
PROTAC CDK4/6/9 degrader 1 prodrug (30 mg/kg; p.o.; daily; 14 days) is well-tolerated in healthy female mice with no observed hematological or organ pathology changes[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:nude mice (8-week-old female; orthotopic cell line-derived xenograft model via injection of 1×106 MDA-MB-231 cells into the fourth mammary fat pad)[1]
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Dosage:30 mg/kg
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Administration:p.o.; daily; 20 days
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Result:Significantly inhibited triple-negative breast cancer tumor growth compared to vehicle and ribociclib-treated groups.
Did not cause significant changes in mouse body weight.
Significantly downregulated CDK4, CDK6, CDK9, and Ki-67 expression in tumor tissues.
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Animal Model:strain not specified (lung metastasis model via tail vein injection of luciferase-labeled TNBC cells)[1]
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Dosage:30 mg/kg
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Administration:p.o.; daily
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Result:Potently suppressed pulmonary colonization of TNBC cells compared to vehicle and ribociclib controls.
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Animal Model:strain not specified (mini patient-derived xenograft model via implantation of fresh patient tumor cell suspension in capsule devices)[1]
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Dosage:30 mg/kg
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Administration:p.o.; daily; 7 days
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Result:Demonstrated significantly lower relative luminescent units (RLU) in tumor cells compared to vehicle and ribociclib groups.
Showed superior tumor inhibition (lower T/C%) compared to the ribociclib group.
Caused no changes in mouse body weight.
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Animal Model:mice (8-week-old female)[1]
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Dosage:30 mg/kg
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Administration:p.o.; daily; 14 days
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Result:Revealed no significant hematological abnormalities compared to vehicle controls.
Showed no notable pathological changes in liver, kidney, heart, spleen, and lung via histological examination.
Chemical Information
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Molecular Weight 1167.44
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Formula C64H86N12O9
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SMILES
O=C(N(C)C)C1=CC2=CN=C(N=C2N1C3CCCC3)NC4=CC=C(C=C4)C(CN5CCN(CC5)CC6CCN(CC6)CC(N7CCN(CC7)C8=CC9=C(C=C8)C(N(C9=O)C(C(N%10COC(CCCCCCCCCCC)=O)=O)CCC%10=O)=O)=O)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PROTAC CDK4/6/9 degrader 1 prodrug Related Classifications
HY-178516 Related Classifications
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