Emiltatug ledadotin
Emiltatug ledadotin (Emi-Le; XMT-1660) is a B7-H4-targeted antibody-drug conjugate (ADC). Emiltatug ledadotin consists of the tumor-specific anti-B7-H4 monoclonal antibody Emiltatug (HY-P990918) and the linker-payload system Ledadotin (HY-177541), with site-specific conjugation achieved via GlycoConnect click chemistry. Emiltatug ledadotin inhibits the growth of B7-H4-positive cancer cells. Emiltatug ledadotin can be used to study advanced solid tumors with B7-H4 overexpression, particularly breast cancer, ovarian cancer, and endometrial cancer.
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- CAS. Nr.: 2855974-40-0
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
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Help & FAQs
Biologische Aktivität
Beschreibung
In Vitro
Emiltatug ledadotin (3 days) potently induces target-dependent cytotoxicity in HEK293-B7-H4 cells, with a payload-based IC50 of 1 nM[2].
Emiltatug ledadotin (3 days) potently induces cytotoxicity in CAMA-1 breast cancer cells, with a payload-based IC50 of 0.052 nM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
In Vivo
Emiltatug ledadotin (2.3/0.075-4.7/0.15 mg/kg; i.v.; single dose) induces complete, sustained tumor regression in the MX-1 breast cancer CDX model following a single intravenous dose across multiple dose levels[2].
Emiltatug ledadotin (2.3/0.075-4.6/0.15 mg/kg; i.v.; single dose) induces complete, sustained tumor regression in the OV2423 ovarian cancer PDX model following a single intravenous dose across multiple dose levels[2].
Emiltatug ledadotin (4.6/0.15 mg/kg; i.v.; single dose) induces potent tumor growth inhibition in the CTG-1692 ovarian cancer PDX model following a single intravenous dose of 4.6/0.15 mg/kg (antibody/payload)[2].
Emiltatug ledadotin (1.5/0.05-4.6/0.15 mg/kg; i.v.; single dose) induces complete, sustained tumor regression in the PD-1 refractory mBR9013 syngeneic breast cancer model following a single intravenous dose across multiple dose levels[2].
Emiltatug ledadotin (4.7/0.15 mg/kg; i.v.; single dose) exhibits antitumor activity in 43% of a diverse panel of breast cancer PDX models following a single intravenous dose of 4.7/0.15 mg/kg (antibody/payload), with activity correlating with B7-H4 expression[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:HSD: Athymic Nude-Foxn1mu (female)[2]
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Dosage:1.5/0.05 mg/kg; 2.3/0.075 mg/kg; 4.7/0.15 mg/kg (antibody/payload)
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Administration:i.v.; single dose
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Result:Induced complete tumor regression at all tested doses.
Resulted in sustained tumor regression with mean tumor volume remaining near 0 mm3 through day 63 post-treatment at the 4.7/0.15 mg/kg dose.
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Animal Model:Crl:NU(Ncr)-Foxn1mu (female)[2]
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Dosage:2.3/0.075 mg/kg; 4.7/0.15 mg/kg (antibody/payload)
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Administration:i.v.; single dose
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Result:Induced complete tumor regression at both tested doses.
Resulted in sustained tumor regression with mean tumor volume remaining near 0 mm3 through day 63 post-treatment at the 4.7/0.15 mg/kg dose.
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Animal Model:BALB/cNj-Foxn1nu/Gpt (female)[2]
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Dosage:2.3/0.075 mg/kg; 4.6/0.15 mg/kg (antibody/payload)
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Administration:i.v.; single dose
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Result:Induced complete tumor regression at both tested doses.
Resulted in sustained tumor regression with mean tumor volume remaining near 0 mm3 through day 70 post-treatment at the 4.6/0.15 mg/kg dose.
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Animal Model:HSD: Athymic Nude-Foxn1mu (female)[2]
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Dosage:4.6/0.15 mg/kg (antibody/payload)
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Administration:i.v.; single dose
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Result:Induced significant tumor growth inhibition, with mean tumor volume remaining near baseline through day 56 post-treatment, while vehicle-treated tumors grew to over 2000 mm3.
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Animal Model:FVB/NJ (female; PD-1 refractory model)[2]
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Dosage:1.5/0.05 mg/kg; 4.6/0.15 mg/kg (antibody/payload)
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Administration:i.v.; single dose
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Result:Induced complete tumor regression at both tested doses.
Resulted in sustained tumor regression with mean tumor volume remaining near 0 mm3 through day 49 post-treatment at the 4.6/0.15 mg/kg dose.
Showed no antitumor activity with anti-PD-1 treatment.
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Animal Model:HSD: Athymic Nude-Foxn1mu (female)[2]
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Dosage:4.7/0.15 mg/kg (antibody/payload)
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Administration:i.v.; single dose
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Result:Achieved median best response (MBR) ≤ -0.3 (≥ 30% tumor shrinkage) in 12/28 (43%) models.
Saw tumor volume reduction in 13/28 (46%) models.
Had more frequent responses in TNBC models (9/15, 60%) than ER-positive models (3/13, 23%).
Showed activity correlating with B7-H4 expression, with 9/13 (69%) models with high tumor proportion score (TPS ≥ 75) achieving MBR ≤ -0.3.
Chemical Information
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CAS. Nr. 2855974-40-0
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SMILES
[Emiltatug ledadotin]
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Synonyms
Emi-Le; XMT-1660
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Emiltatug ledadotin Related Classifications
HY-177542 Related Classifications
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