Calotatug ginistinag
Based on 1 Customer Validation
Calotatug ginistinag (XMT-2056) is an antibody-drug conjugate (ADC) targeting HER2, linked to a payload composed of XMT-1519 conjugate-1 (HY-148067) and STING agonist-20 (HY-148068). Calotatug ginistinag activates the STING signaling pathway in tumor cells and tumor-resident immune cells, induces the production of type I interferons and cytokines (CXCL10, IFN-β, IL-6, TNF-α, triggers innate anti-tumor immune responses, and exerts a bystander effect. Calotatug ginistinag exhibits efficacy against HER2-expressing cancer cells in co-culture with PBMCs. Calotatug ginistinag induces tumor regression and reduces systemic inflammation in various tumor models. Combination treatment with Calotatug ginistinag, Trastuzumab (HY-P9907) and T-DXd (HY-138298) yields benefits. Calotatug ginistinag can be used in studies related to HER2-expressing solid tumors such as breast cancer, gastric cancer and ovarian cancer.
For research use only. We do not sell to patients.
- Purity: 95.94%
- CAS No.: 2847102-44-5
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Storage:
-80°C, protect from light
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Biological Activity
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HER2 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MDA-MB-175-VII | IC50 |
0.38 nM
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Immune-mediated killing of human MDA-MB-175-VII-NR HER2-low breast cancer cells in PBMC cocultures, with 20 minutes pre-incubation with MDA-MB-175-VII-NR cells and 84 hours total incubation, quantified via live-cell imaging of red fluorescence.
Immune-mediated killing of human MDA-MB-175-VII-NR HER2-low breast cancer cells in PBMC cocultures, with 20 minutes pre-incubation with MDA-MB-175-VII-NR cells and 84 hours total incubation, quantified via live-cell imaging of red fluorescence.
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40029253 |
Calotatug ginistinag induces cytokine production and kills cancer cells in PBMC co-culture systems with cancer cells that have low HER2 expression[1].
Calotatug ginistinag (24 h) directly activates STING in HER2-positive HCC1954 breast cancer cells and induces CXCL10 production, with an EC50 of 2.67 nM payload[2].
Calotatug ginistinag (24 h) induces antigen-dependent, Fcγ receptor-mediated STING activation in THP1 monocytes when co-cultured with HER2-positive SKOV3 ovarian cancer cells[2].
Calotatug ginistinag (24 h) induces antigen-dependent, Fcγ receptor-mediated STING activation in THP1 monocytes cultured on recombinant HER2 protein-coated plates[2].
Calotatug ginistinag (0.01-1000 nM payload; 84 h) potently induces immune-mediated killing of HER2-positive SKBR3-NR breast cancer cells in a PBMC co-culture system, with an IC50 of 0.023 nM for its payload[2].
Calotatug ginistinag (0.01-1000 nM payload; 84 h) induces immune-mediated killing of HER2-low expressing MDA-MB-175-VII-NR breast cancer cells in a PBMC co-culture system, with an IC50 of 0.38 nM for its payload[2].
Calotatug ginistinag (0.01-10 nM payload; 84 h) induces immune-mediated killing of HER2-negative MDA-MB-231-NR breast cancer cells, and this effect occurs only in the presence of HER2-positive SKBR3 breast cancer cells and peripheral blood mononuclear cells (PBMCs). The IC50 value of its payload is 0.25 nM at a 1:1 ratio and 0.34 nM at a 1:4 ratio[2].
Calotatug ginistinag (0.01-1000 nM payload; 24 h) induces concentration-dependent production of STING pathway cytokines (CXCL10, IFN-β, IL-6, TNF-α) in a co-culture system of SKBR3-NR breast cancer cells and PBMCs, with EC50 values of the payload ranging from 0.17 to 0.46 nM[2].
Calotatug ginistinag (0.01-1000 nM payload; 24 h) induces concentration-dependent expression of STING pathway cytokines (CXCL10, IFN-β, IL-6, TNF-α) in a co-culture system of MDA-MB-175-VII-NR breast cancer cells and PBMCs, with EC50 values of the payload ranging from 0.30 to 0.76 nM[2].
Calotatug ginistinag specifically binds to HER2-positive HCC1954 breast cancer cells, with a binding affinity comparable to that of unconjugated HT19 antibody[2].
Calotatug ginistinag specifically binds to HER2-positive SKOV3 ovarian cancer cells, with a binding affinity comparable to that of the unconjugated HT19 antibody and the Fc mutant XMT-2056[2].
Calotatug ginistinag binds to Fcγ-RI, whereas the Fc mutant XMT-2056 lacks Fcγ-RI binding activity[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Calotatug ginistinag (1-3 mg/kg; intravenous injection; single administration) induces complete and sustained tumor regression in HER2-expressing HCC1954 and SNU-5 xenograft models, with superior efficacy to free STING agonists[2].
Calotatug ginistinag (0.2 mg/kg; intravenous injection; single administration) enhances the anti-tumor activity of Trastuzumab (HY-P9907) in SNU-5 xenografts[2].
Calotatug ginistinag (1-3 mg/kg; intravenous injection; single administration) induces tumor growth delay in Trastuzumab-resistant JIMT-1 xenografts, with better efficacy than free STING agonists[2].
Calotatug ginistinag (0.2 mg/kg; intravenous injection; once weekly; 3 doses total) enhances the anti-tumor activity of Trastuzumab in SKOV3 xenografts[2].
Combination of calotatug ginistinag (1 mg/kg; intravenous injection; single dose) with T-DXd (HY-138298) induces durable tumor regression in a Trastuzumab-resistant JIMT-1 breast cancer xenograft model[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CB.17 SCID (female; subcutaneous inoculation with 1×107 SKOV3 cells in 50% Matrigel)[2]
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Dosage:Single agent (single dose): 0.3 mg/kg, 1 mg/kg, 3 mg/kg;
Single agent (weekly × 3): 0.067 mg/kg, 0.17 mg/kg, 0.3 mg/kg;
Trastuzumab (weekly × 3): the ADC 0.2 mg/kg + Trastuzumab 2 mg/kg -
Administration:Single agent (single dose): Intravenous injection (i.v.); single dose; Single agent (weekly × 3): Intravenous injection (i.v.); weekly × 3 doses; Trastuzumab: the ADC: Intravenous injection (i.v.), weekly × 3 doses; Trastuzumab: Intraperitoneal injection (i.p.), weekly × 3 doses
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Result:Induced complete and sustained tumor regressions with a single 1 mg/kg or 3 mg/kg dose.
Resulted in partial and complete responses with three weekly 0.067 mg/kg doses.
Activated STING pathway in both tumor cells and murine host cells with a single 0.3 mg/kg dose.
Induced transient elevations in serum cytokines (CXCL10, IL-6, MIP-1β, RANTES, CXCL9), which were 1.5- to 10-fold lower than those induced by a free diABZI STING agonist.
Elevated murine mRNA levels of immune cell markers CD68 and CD45 in tumors 72 hours post-treatment.
Increased tumor infiltration of CD68+ and CD45+ cells.
Upregulated mPD-L1 staining.
Showed improved antitumor activity in combination with trastuzumab over either single agent.
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Animal Model:SCID beige (female; subcutaneous inoculation with 1×107 HCC1954 cells in 50% Matrigel)[2]
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Dosage:1 mg/kg (single dose); 3 mg/kg (single dose)
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Administration:i.v.; single dose
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Result:Induced complete and sustained tumor regressions with a single 1 mg/kg or 3 mg/kg dose.
Outperformed a free diABZI STING agonist administered at a 100-fold higher payload dose equivalent.
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Animal Model:CB.17 SCID (female; subcutaneous inoculation with 1×107 SNU-5 cells in 50% Matrigel)[2]
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Dosage:Single agent: 1 mg/kg, 3 mg/kg; Trastuzumab: the ADC 0.2 mg/kg + Trastuzumab 2 mg/kg
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Administration:Single agent: Intravenous injection (i.v.); single dose; Trastuzumab: the ADC: Intravenous injection (i.v.), single dose; Trastuzumab: Intraperitoneal injection (i.p.), single dose
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Result:Induced complete and sustained tumor regressions with a single 1 mg/kg or 3 mg/kg dose.
Outperformed a free diABZI STING agonist administered at a 100-fold higher payload dose equivalent.\nShowed improved antitumor activity in combination with trastuzumab over either single agent.
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Animal Model:CB.17 SCID (female; subcutaneous inoculation with 1×107 JIMT-1 cells in 50% Matrigel)[2]
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Dosage:Single agent: 1 mg/kg, 3 mg/kg; the ADC 0.3 mg/kg + Trastuzumab 3 mg/kg; the ADC 1 mg/kg + T-DXd 3 mg/kg
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Administration:Single agent: Intravenous injection (i.v.); single dose
Trastuzumab: the ADC: Intravenous injection (i.v.), weekly × 3 doses; Trastuzumab: Intraperitoneal injection (i.p.), weekly × 3 doses
T-DXd: the ADC: Intravenous injection (i.v.), single dose; T-DXd: Intravenous injection (i.v.), weekly × 2 doses (1 week apart) -
Result:Showed improved antitumor activity in combination with trastuzumab over either single agent.
Induced durable tumor regressions when 3 mg/kg XMT-2056 was combined with trastuzumab deruxtecan (T-Dxd).
Induced tumor growth delay with a single 1 mg/kg or 3 mg/kg dose.
Outperformed a free diABZI STING agonist administered at a 100-fold higher payload dose equivalent.
Chemical Information
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CAS No. 2847102-44-5
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Appearance Liquid
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Color Colorless to light yellow
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SMILES
[Calotatug ginistinag]
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Synonyms
XMT-2056
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Shipping
Shipping with dry ice.
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Storage
-80°C, protect from light
Purity & Documentation
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Data Sheet (285 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[2]. Bukhalid RA, et al. XMT-2056, a HER2-Directed STING Agonist Antibody-Drug Conjugate, Induces Innate Antitumor Immune Responses by Acting on Cancer Cells and Tumor-Resident Immune Cells. Clinical cancer research : an official journal of the American Association for Cancer Research. 2025 May 01;31(9):1766-1782. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Calotatug ginistinag Related Classifications
HY-164919 Related Classifications
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- Calotatug ginistinag
- 2847102-44-5
- XMT-2056
- XMT2056
- XMT 2056
- Antibody-Drug Conjugates (ADCs)
- EGFR
- STING
- IFNAR
- TNF Receptor
- Interleukin Related
- CXCR
- THP1 monocytes
- PD-L1
- Fcγ receptor
- SKOV3 ovarian cancer cells
- SKBR3-NR breast cancer cells
- PBMC
- HCC1954 breast cancer cells
- MDA-MB-175-VII-NR breast cancer cells
- HER2
- Inhibitor
- inhibitor
- inhibit