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  3. Pomalidomide 5'-pip-acid

Pomalidomide 5'-pip-acid is an E3 ligase ligand-linker conjugate derived from the molecular glue Pomalidomide (HY-10984), which can be used to synthesize the dual-target PROTAC degrader PROTAC CBP/p300/BRD4 Degrader-1 (HY-181758) targeting CBP/p300 and BRD4. Pomalidomide 5'-pip-acid shows anti-proliferative activity against cancer cells with an IC50 of 2.73 nM. Pomalidomide 5'-pip-acid induces anti-proliferative effects in cancer cells. Pomalidomide 5'-pip-acid is applicable to research related to prostate cancer and colorectal cancer.

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Pomalidomide 5'-pip-acid

Pomalidomide 5'-pip-acid Chemical Structure

CAS No. : 2467965-70-2

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Description

Pomalidomide 5'-pip-acid is an E3 ligase ligand-linker conjugate derived from the molecular glue Pomalidomide (HY-10984), which can be used to synthesize the dual-target PROTAC degrader PROTAC CBP/p300/BRD4 Degrader-1 (HY-181758) targeting CBP/p300 and BRD4. Pomalidomide 5'-pip-acid shows anti-proliferative activity against cancer cells with an IC50 of 2.73 nM. Pomalidomide 5'-pip-acid induces anti-proliferative effects in cancer cells. Pomalidomide 5'-pip-acid is applicable to research related to prostate cancer and colorectal cancer[1].

In Vitro

Derivatives of Pomalidomide 5'-pip-acid potently inhibit the proliferation of human prostate cancer cell line PC-3 in vitro, with IC50 values ranging from 2.73 nM to 24.77 nM. Among them, the most active compound has an IC50 of 2.73 nM[1].
Derivatives of Pomalidomide 5'-pip-acid (5-20 nM; 12 h) effectively degrade BRD4 protein in human prostate cancer PC-3 cells at concentrations of 5 nM and 20 nM after 12 h of treatment[1].

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

In Vivo

Derivative of Pomalidomide 5'-pip-acid (0.1-0.2 mg/kg; i.p.; once every 2 days; 24 days) achieve dose-dependent tumor growth inhibition in the PC-3 xenograft mouse model, with a maximum inhibition rate of up to 81.5% at the dose of 0.2 mg/kg, and exhibit favorable preliminary safety profiles[1].

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

Molecular Weight

385.37

Formula

C19H19N3O6

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C1CCN(C2=CC3=C(C(N(C(CC4)C(NC4=O)=O)C3=O)=O)C=C2)CC1)O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, protect from light, stored under nitrogen

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

Purity & Documentation
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  • 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.

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Product Name:
Pomalidomide 5'-pip-acid
Cat. No.:
HY-W877997
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