Rolinsatamab talirine
Rolinsatamab talirine (ABBV 176) is a prolactin receptor (PRLR)-targeting antibody-drug conjugate (ADC), compoused of Rolinsatamab (HY-P99238) and SGD-1882 (HY-101127). Rolinsatamab talirine binds to PRLR to deliver a cytotoxin to tumor cells. Rolinsatamab talirine induces DNA damage, and exhibits cytotoxicity against multiple breast tumor models, including triple negative and low PRLR-expressing models. Rolinsatamab talirine demonstrates enhanced anti-tumor activity in several breast cancer models. Rolinsatamab talirine can be used for the research of breast cancer, hepatocellular carcinoma, ovarian cancer, endometrial cancer, prostate cancer, colorectal cancer, adrenocortical carcinoma, and solid tumors.
For research use only. We do not sell to patients.
- CAS No.: 2095467-44-8
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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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
Biological Activity
Rolinsatamab talirine binds to recombinant human and cynomolgus PRLR extracellular domains with high affinity, with KD values of 1.0 nM and 0.7 nM respectively[1].
Rolinsatamab talirine (0.01-100 nM) binds specifically to cell surface PRLR on PRLR-expressing human tumor cell lines (T47D, MCF7) and human PRLR-overexpressing HEK-293 cells, with no appreciable binding to PRLR-negative HEK-293 vector control cells[1].
Rolinsatamab talirine (144 h) potently inhibits the growth of multiple PRLR-expressing human tumor cell lines (including breast, prostate, endometrial, ovarian, colorectal, and liver) with IC50 values ranging from 0.0055 nM to 8.6 nM, and does not affect the viability of normal human cell lines or PRLR-negative tumor cell lines at concentrations up to 22 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Rolinsatamab talirine (0.01-0.3 mg/kg; i.p.; Q7D × 3) induces durable tumor regression in mouse CTG-0869 triple negative breast cancer PDX models[1].
Rolinsatamab talirine (0.1-0.2 mg/kg; i.p.; Q7D × 3; single dose) induces significant tumor regression in mouse CTG-0670 triple negative breast cancer PDX models[1].
Rolinsatamab talirine (0.2 mg/kg; i.p.; Q7D × 3) significantly improves survival of mice bearing HepG2 hepatocellular carcinoma xenografts[1].
Rolinsatamab talirine (0.2 mg/kg; i.p.; Q7D × 3) improves survival of mice bearing HuH-7 LOT hepatocellular carcinoma xenografts, with enhanced efficacy when combined with Veliparib (HY-10129)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female SCID Beige mice implanted subcutaneously with BT-474 cells[1]
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Dosage:0.5 mg/kg
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Administration:i.p.; single dose
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Result:Induced significant tumor regression.
Caused no significant impact on mouse body weight or gross physiologic changes.
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Animal Model:Female SCID Beige mice implanted subcutaneously with CTG-0869 cells[1]
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Dosage:0.01; 0.03; 0.1; 0.2; 0.3 mg/kg
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Administration:i.p.; Q7D × 3
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Result:Induced durable tumor regression at doses of 0.3 mg/kg, 0.2 mg/kg, and 0.1 mg/kg.
Caused tumors treated with 0.1 mg/kg to begin regrowing by day 63.
Caused minimal tumor growth delay at 0.03 mg/kg.
Showed no reported efficacy at 0.01 mg/kg.
Caused no significant impact on mouse body weight or gross physiologic changes.
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Animal Model:Female SCID Beige mice implanted subcutaneously with CTG-0670 cells[1]
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Dosage:0.1; 0.2 mg/kg
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Administration:i.p.; Q7D × 3; single dose
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Result:Induced significant tumor regression (p ≤ 0.05) at 0.2 mg/kg and 0.1 mg/kg administered Q7D × 3.
Showed high potency (p ≤ 0.05) at single 0.1 mg/kg dose.
Caused no significant impact on mouse body weight or gross physiologic changes.
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Animal Model:SCID Beige (female, expanded panel of 11 human breast cancer patient-derived xenografts implanted subcutaneously with 0.2 mL of a 1:1 mixture of tumor brie and Matrigel)[1]
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Dosage:0.5 mg/kg; 0.2 mg/kg
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Administration:i.p.; Q7D × 3
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Result:Achieved high tumor growth inhibition.
Induced significant tumor regression.
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Animal Model:SCID mice (female) implanted subcutaneously with HepG2 cells[1]
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Dosage:0.2 mg/kg
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Administration:i.p.; Q7D × 3
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Result:Induced significant tumor growth delay and improved survival compared to vehicle (p < 0.001) and control PBD ADC (p < 0.005).
Caused no significant impact on mouse body weight or gross physiologic changes.
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Animal Model:SCID mice (female) implanted subcutaneously with HuH-7 LOT cells[1]
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Dosage:0.2 mg/kg
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Administration:i.p.; Q7D × 3
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Result:Improved mouse survival as monotherapy.
Further increased survival when combined with Veliparib.
Caused no significant impact on mouse body weight or gross physiologic changes.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2095467-44-8
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SMILES
[Rolinsatamab talirine]
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Synonyms
ABBV 176
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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
[1]. Anderson MG, et al. ABBV-176, a PRLR antibody drug conjugate with a potent DNA-damaging PBD cytotoxin and enhanced activity with PARP inhibition. BMC Cancer. 2021;21(1):681. Published 2021 Jun 9. [Content Brief]
[2]. Lemech C, et al. A first-in-human, phase 1, dose-escalation study of ABBV-176, an antibody-drug conjugate targeting the prolactin receptor, in patients with advanced solid tumors. Invest New Drugs. 2020;38(6):1815-1825. [Content Brief]
[3]. Mukherjee A, et al. Targeted Therapy in Breast Cancer: Advantages and Advancements of Antibody-Drug Conjugates, a Type of Chemo-Biologic Hybrid Drugs. Cancers (Basel). 2024;16(20):3517. Published 2024 Oct 17. [Content Brief]
[4]. Chervin AS, et al. ABBV-184: A Novel Survivin-specific TCR/CD3 Bispecific T-cell Engager is Active against Both Solid Tumor and Hematologic Malignancies. Mol Cancer Ther. 2023;22(8):903-912. [Content Brief]
[5]. Zhang J, et al. The immunotoxin targeting PRLR increases tamoxifen sensitivity and enhances the efficacy of chemotherapy in breast cancer. J Exp Clin Cancer Res. 2024;43(1):173. Published 2024 Jun 20. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Rolinsatamab talirine Related Classifications
HY-P99881 Related Classifications
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