Product Data Sheet
Polθ-IN-9
Catalog No. A38498
Polθ-IN-9 is a selective inhibitor of Pol θ polymerase, demonstrating an IC50 value of 9.6 nM and a Kd of 47.5 nM, with no significant inhibitory effects on other human DNA polymerases such as Pol α, Pol ε, Pol γ, Pol λ, and Pol μ. This compound exhibits potent antiproliferative activity in DLD1 BRCA2 knockout cells (IC50 = 2.9 μM) and MDA-MB-436 cells (IC50 = 4.9 μM), while also increasing DNA damage and γH2AX levels. In addition, Polθ-IN-9 has shown to inhibit tumor growth in conjunction with Olaparib in the MDA-MB-436 xenograft model, making it a valuable tool for studying homologous recombination-deficient cancers, including breast cancer.
Chemical Information
| Catalog Num | A38498 |
|---|---|
| M. Wt | 624.04 |
| Formula | C30H31ClF5N5O2 |
| Purity | >98% |
| Storage | at -20 °C 3 years (powder form); at -20 °C 6 months (Solution base) |
| CAS No. | 3050552-13-8 |
| Synonyms | |
| SMILES | COCCN1CCN(CC1)C2=CC=C3N([C@@H](CC3=C2)C(N(C)C4=CC(Cl)=C(C=C4F)F)=O)C5=CC(C(F)(F)F)=CC(C)=N5 |
Biological Activity
| Description | Polθ-IN-9 is a selective inhibitor of Pol θ polymerase, demonstrating an IC50 value of 9.6 nM and a Kd of 47.5 nM, with no significant inhibitory effects on other human DNA polymerases such as Pol α, Pol ε, Pol γ, Pol λ, and Pol μ. This compound exhibits potent antiproliferative activity in DLD1 BRCA2 knockout cells (IC50 = 2.9 μM) and MDA-MB-436 cells (IC50 = 4.9 μM), while also increasing DNA damage and γH2AX levels. In addition, Polθ-IN-9 has shown to inhibit tumor growth in conjunction with Olaparib in the MDA-MB-436 xenograft model, making it a valuable tool for studying homologous recombination-deficient cancers, including breast cancer. |
|---|
RETURN POLICY
Adooq’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
Adooq’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
SHIPPING AND STORAGE
Adooq products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Adooq Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Adooq products are stable under the recommended conditions.
Adooq products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Adooq Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Adooq products are stable under the recommended conditions.
