2. Immunology/Inflammation
  3. CD47
  4. Evorpacept

Evorpacept  (Synonyms: ALX148)

Cat. No.: HY-P99950 Purity: 99.75%
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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.

For research use only. We do not sell to patients.

CAS No. : 2484949-51-9

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Description

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

IC50 & Target

CD47
In Vitro

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 Related Antibodies
In Vivo

Evorpacept (ALX148) (i.p., twice weekly for 3 weeks) combined with obinutuzumab, trastuzumab or rituximab markedly strengthened tumor suppression in corresponding NOD-SCID female xenograft models; rituximab co-treatment additionally prolonged mouse survival[1].
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.

Animal Model: C57BL/6 (female, 6-8 weeks old, subcutaneous implantation of 0.5×106 MC38 tumor cells)[1]
Dosage: 30 mg/kg
Administration: i.p.; two doses; 10 days apart
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.
Animal Model: BALB/c (female, 6-8 weeks old, subcutaneous implantation of 0.5×106 CT26 tumor cells)[1]
Dosage: 30 mg/kg
Administration: i.p.; single dose
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.
Animal Model: BALB/c (female, 6-8 weeks old, subcutaneous implantation of 0.5×106 CT26-M/H HER2 tumor cells)[1]
Dosage: 10, 30 mg/kg
Administration: i.p.; single dose
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.
Application

ELISA, FACS, Functional assay
Conjugated

Unconjugated
Reconsititution

The product can be reconstituted/diluted with sterile PBS or saline.
Molecular Weight

76.61 kDa

CAS No.
Appearance

Liquid

Color

Colorless to light yellow

SMILES

[Evorpacept]
Shipping

Shipping with dry ice.
Formulation

Please refer to the lot-specific COA for specific buffer information.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Format
  • Homo sapiens SIRPA (signal regulatory protein alpha, SHPS1, SIRP, SIRPalpha)-IGHG1 (Fc (Fragment constant)
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References
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  • 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:

Evorpacept2484949-51-9ALX148ALX 148ALX-148CD47Cluster of Differentiation 47MER6OA3gastric cancerSIRPαtumor-associated macrophagesdendritic cellacute myeloid leukemiab-cell mantle cell lymphomaT cellcolon carcinomab-cell lymphomaInhibitorinhibitorinhibit

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