2. Cell Cycle/DNA Damage
  3. DNA/RNA Synthesis
  4. RTx-303

RTx-303 is an orally active, selective DNA polymerase θ (Polθ) inhibitor (IC50 = 5.1 nM). RTx-303 exhibits significantly high cellular potency and strongly potentiates PARPi in BRCA1/2 mutant cells and patient-derived xenograft models. RTx-303 can be used for the study of BRCA2-mutated breast cancer.

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RTx-303

RTx-303 Chemical Structure

CAS No. : 3035072-99-9

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RTx-303 Related Antibodies

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Description

RTx-303 is an orally active, selective DNA polymerase θ (Polθ) inhibitor (IC50 = 5.1 nM). RTx-303 exhibits significantly high cellular potency and strongly potentiates PARPi in BRCA1/2 mutant cells and patient-derived xenograft models. RTx-303 can be used for the study of BRCA2-mutated breast cancer[1].

Application

1. This compound can be used as a tracer.
2. This compound can be used as an internal standard for quantitative analysis by NMR, GC-MS, or LC-MS.

In Vitro

RTx-303 significantly inhibits Polθ-pol activity, but has no significant effect on other DNA polymerases (such as Polβ, Polη, Polγ, etc)[1].
RTx-303 (10 μM) shows no significant inhibition of most kinases (% activity >90%), and only mild inhibition of a few kinases, such as PASK (75% activity) and ATR/ATRIP (77% activity)[1].
RTx-303 shows an IC50 of 81.2 nM against HRD cells (HCT116 BRCA2-/-) and >1280 nM against HR-proficient cells (HCT116 BRCA2+/+), demonstrating >100-fold selectivity[1].
RTx-303 (5 μM, 5 days) in combination with Olaparib (HY-10162) significantly reduces the IC50 of ID8 BRCA2-/- cells (from 2 μM to 0.12 μM) and restores Olaparib sensitivity in PARPi-resistant cells[1].

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

RTx-303 Related Antibodies
In Vivo

RTx-303 (60 mg/kg, p.o., twice daily for 28-42 days) effectively inhibits the growth of BRCA2-mutated tumors in mouse models, whether used alone or in combination with PARPi, and no significant weight loss is observed, indicating a high safety profile[1].
RTx-303 (60 mg/kg, p.o., twice daily for 56 days), in combination with Olaparib, can prevent acquired resistance to PARPi in BRCA1-mutant tumors in MDA-MB-436 xenograft mice[1].

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

Animal Model: For the BR-05-0566 (BR-05-0568) BRCA2 mutant PDX study, ∼ 30 mm3 tumor fragment was implanted subcutaneously into female BALB/c mice 6-8 weeks old[1].
Dosage: 60 mg/kg
Administration: P.o., twice daily for 28 days (BR-05-0566) to 42 days (BR-05-0568)
Result: BR-05-0566 model: Significantly inhibited tumor growth (compared to the vehicle group); combined with olaparib, it led to tumor regression; tumor volume reduction >80% in the combination group.
BR-05-0568 model: Combined with talazoparib, it resulted in 100% complete tumor elimination.
No significant weight loss was observed in any group.
Animal Model: 10 × 106 MDA-MB-436 (bearing BRCA1-Mutant) cells were injected with Matrigel subcutaneously into female BALB/c mice, 6-8 weeks old[1].
Dosage: 60 mg/kg
Administration: P.o., twice daily for 56 days
Result: Treated with Olaparib, tumors regressed rapidly and there was no recurrence.
Molecular Weight

569.49

Formula

C24H22D3F7N4O4
CAS No.
Unlabeled CAS
SMILES

CN(C)C[C@@H](O)CN(C1=O)CCN1C2=C(OC(N(C([2H])([2H])[2H])C3=CC=C(F)C=C3)=O)C(C(F)(F)F)=CC(C(F)(F)F)=C2
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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RTx-303 Related Classifications

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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:

RTx-3033035072-99-9RTx303RTx 303DNA/RNA SynthesisDNA polymerase thetaPolθBRCA mutant tumorsBreast cancerPatient-derived xenograftPDXCell-derived xenograftCDXInhibitorinhibitorinhibit

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