2. Antibody-drug Conjugate/ADC Related
  3. Antibody-Drug Conjugates (ADCs)
  4. 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.

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Rolinsatamab talirine

Rolinsatamab talirine Chemical Structure

CAS No. : 2095467-44-8

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Rolinsatamab talirine Related Antibodies

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Description

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[1][2][3][4][5].

In Vitro

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 Related Antibodies
In Vivo

Rolinsatamab talirine (0.5 mg/kg; i.p.; single dose) induces significant regression of established BT-474.FP2 breast cancer xenografts in female SCID Beige mice[1].
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.

Animal Model: Female SCID Beige mice implanted subcutaneously with BT-474 cells[1]
Dosage: 0.5 mg/kg
Administration: i.p.; single dose
Result: Induced significant tumor regression.
Caused no significant impact on mouse body weight or gross physiologic changes.
Animal Model: Female SCID Beige mice implanted subcutaneously with CTG-0869 cells[1]
Dosage: 0.01; 0.03; 0.1; 0.2; 0.3 mg/kg
Administration: i.p.; Q7D × 3
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.
Animal Model: Female SCID Beige mice implanted subcutaneously with CTG-0670 cells[1]
Dosage: 0.1; 0.2 mg/kg
Administration: i.p.; Q7D × 3; single dose
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.
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]
Dosage: 0.5 mg/kg; 0.2 mg/kg
Administration: i.p.; Q7D × 3
Result: Achieved high tumor growth inhibition.
Induced significant tumor regression.
Animal Model: SCID mice (female) implanted subcutaneously with HepG2 cells[1]
Dosage: 0.2 mg/kg
Administration: i.p.; Q7D × 3
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.
Animal Model: SCID mice (female) implanted subcutaneously with HuH-7 LOT cells[1]
Dosage: 0.2 mg/kg
Administration: i.p.; Q7D × 3
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.
Clinical Trial
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[Rolinsatamab talirine]
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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:

Rolinsatamab talirine2095467-44-8ABBV 176ABBV176ABBV-176Antibody-Drug Conjugates (ADCs)Antibody-Drug Conjugatesbreast tumor modelsprolactin receptorpoly-ADP ribose polymerase inhibitorPRLRMCF7T47Dpyrrolobenzodiazepine dimer cytotoxintriple negative breast cancerSCID Beige miceHEK-293Inhibitorinhibitorinhibit

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