Evorpacept
Based on 1 Customer Validation
Evorpacept (ALX148) is a high-affinity CD47-blocking fusion protein with an inactive human immunoglobulin Fc region. Evorpacept binds to CD47, blocks the interaction of the CD47-SIRPα immune checkpoint, and inhibits the binding of wild-type SIRPα to CD47. Evorpacept is applicable to research related to acute myeloid leukemia.
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- 純度: 99.75%
- CAS 番号: 2484949-51-9
- 分子量:76.61 kDa
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保管条件:
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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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
CD47
Evorpacept (ALX148) binds to the CD47-ECD of humans, cynomolgus monkeys, mice and rats with high affinity, and its affinity for human CD47 reaches the picomolar level at 25°C (Kd = 140 pM)[1].
Evorpacept (20 nM; 15 min on ice) binds to CD47 expressed on the surface of OE19, DLD-1, MM1.R, Raji, Z138, Daudi, CT26, and MC38 tumor cells[1].
Evorpacept (12.5 nM; 15 min on ice) blocks the binding of wild-type SIRPα to CD47 on Jurkat tumor cells by over 90%[1].
Evorpacept binds to human FcRn at 25°C, with a Kd of approximately 580 nM[1].
Evorpacept, when combined with Trastuzumab (HY-P9907), Cetuximab (HY-P9905), Daratumumab (HY-P9915) or Obinutuzumab (HY-P9910), enhances the antibody-dependent phagocytosis of OE19, DLD-1, MM1.R and Daudi tumor cells by human monocyte-derived macrophages[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Evorpacept (ALX148) (30 mg/kg; i.p.; two doses; 10 days apart) enhances the antitumor efficacy of anti-PD-L1 in female C57BL/6 mice bearing MC38 colon carcinoma, driving significant tumor growth inhibition, prolonged survival, and a robust intratumoral adaptive immune response[1].
Evorpacept (ALX148) (30 mg/kg; i.p.; single dose) modulates innate and adaptive immune responses, and enhances the antitumor efficacy of anti-PD-1 in female BALB/c mice bearing CT26 colon carcinoma, driving significant tumor growth inhibition, prolonged survival, and reduced immune suppression in the tumor microenvironment[1].
Evorpacept (ALX148) (10-30 mg/kg; i.p.; single dose) achieves dose-dependent CD47 occupancy in splenic and tumor tissues of female BALB/c mice bearing CT26-M/H HER2 tumors, with 30 mg/kg achieving near-maximal tumor CD47 occupancy and prolonged systemic exposure[1].
Evorpacept (ALX148) (10-30 mg/kg; i.v.; single dose) achieves complete CD47 occupancy on circulating T lymphocytes, with dose-dependent persistence of occupancy in female cynomolgus monkeys[1].
Evorpacept (ALX148) (i.p.; two doses; 5 days apart) in combination with anti-4-1BB significantly enhances survival in female BALB/c mice bearing CT26 colon carcinoma, compared to PBS[1].
Evorpacept synergizes with multiple antibody agents to boost tumor suppression and survival in diverse tumor models, whereas its monotherapy shows weak efficacy; it also reprograms CT26 tumor-associated macrophages into antitumor phenotypesy[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (female, 6-8 weeks old, subcutaneous implantation of 0.5×106 MC38 tumor cells)[1]
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Dosage:30 mg/kg
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Administration:i.p.; two doses; 10 days apart
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Result:Showed minimal single-agent tumor growth inhibition.
Resulted in significantly enhanced tumor growth inhibition compared to anti-PD-L1 alone.
Significantly increased survival compared to PBS.
Significantly increased tumor-infiltrating CD8+ T cells, CD4+ T cells, effector memory CD8+ T cells, effector memory CD4+ T cells, IFNγ-expressing CD8+ T cells, and granzyme B-expressing CD8+ T cells compared to vehicle control.
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Animal Model:BALB/c (female, 6-8 weeks old, subcutaneous implantation of 0.5×106 CT26 tumor cells)[1]
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Dosage:30 mg/kg
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Administration:i.p.; single dose
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Result:Showed minimal single-agent tumor growth inhibition.
Resulted in significantly enhanced tumor growth inhibition compared to anti-PD-1 alone.
Significantly increased survival.
Resulted in a nearly 3-fold increase in the ratio of M1 to M2 tumor-associated macrophages and a 4-fold decrease in splenic CD8- dendritic cells (DCs) compared to vehicle control.
Upregulated the activation marker CD86 on splenic CD8+ and CD8- DCs, increased splenic effector memory CD4+ T cells, central memory CD4+ T cells, central memory CD8+ T cells, KLRG1 expression on CD8+ T cells, and AH1-specific tumor-reactive CD8+ T cells compared to vehicle control.
Resulted in a 2.5-fold increase in the M1 to M2 macrophage ratio, a 1.7-fold decrease in monocytic myeloid-derived suppressor cells, a 2.2-fold increase in splenic CD8+ DCs, and increased IFNγ expression in tumor-infiltrating CD8+ T cells.
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Animal Model:BALB/c (female, 6-8 weeks old, subcutaneous implantation of 0.5×106 CT26-M/H HER2 tumor cells)[1]
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Dosage:10, 30 mg/kg
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Administration:i.p.; single dose
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Result:Achieved dose-dependent CD47 occupancy in splenic and tumor tissues of female BALB/c mice bearing CT26-M/H HER2 tumors, with 30 mg/kg achieving near-maximal tumor CD47 occupancy and prolonged systemic exposure.
Unconjugated
The product can be reconstituted/diluted with sterile PBS or saline.
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Homo sapiens SIRPA (signal regulatory protein alpha, SHPS1, SIRP, SIRPalpha)-IGHG1 (Fc (Fragment constant)
ELISA, FACS, Functional assay
化学情報
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CAS 番号 2484949-51-9
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性状 Liquid
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分子量 76.61 kDa
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Color Colorless to light yellow
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SMILES
[Evorpacept]
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別名
ALX148
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輸送条件
Shipping with dry ice.
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Formulation
Please refer to the lot-specific COA for specific buffer information.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
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データシート (267 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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Inhibitory Antibodies User Guide (603 KB)
参考文献
[1]. Kauder SE, et al. ALX148 blocks CD47 and enhances innate and adaptive antitumor immunity with a favorable safety profile. PLoS One. 2018;13(8):e0201832. Published 2018 Aug 22. [Content Brief]
[3]. Kim TM, et al. Evorpacept plus rituximab for the treatment of relapsed or refractory non-Hodgkin lymphoma: results from the phase I ASPEN-01 study. Haematologica. 2025;110(9):2102-2112. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Evorpacept 関連分類
HY-P99950 関連分類
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