Art. -Nr.: HY-P990901

Biologically Validated

Aplitabart

(Synonyms: IGM-8444)

Kundenbewertung

Based on 1 Customer Validation

Aplitabart (IGM-8444) is a pentameric IgM death receptor 5 (DR5) agonist antibody with a K_D of 85 nM and an apparent affinity of 11 pM. Aplitabart induces DR5 multimerization, thereby triggering cancer cell apoptosis via the extrinsic apoptotic pathway apoptosis. Aplitabart is applicable to cancer-related research such as colorectal cancer and gastric cancer.

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Reinheit: 97.024%
CAS. Nr.: 2796349-94-3
Molecular Weight:871.57 kDa

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Aplitabart Chemical Structure

CAS. Nr.: 2796349-94-3

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- Isotype
- Recommend Isotype Controls
- Species Reactivity
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
- Gene ID
- Accession
- Conjugated
- Reconsititution
- Format
- Anwendung
- Verified Bioactivity
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Isotype

Human IgM-kappa_Jchain

Recommend Isotype Controls

Human IgM, Isotype Control

Species Reactivity

Human

IC₅₀ & Target

DR5

Alle TNF Receptor Isoform-spezifische Produkte anzeigen :

In Vitro

IGM-8444 potently binds to Colo205 colorectal cancer cells (EC₅₀ = 170 ng/mL) and H-EMC-SS chondrosarcoma cells (EC₅₀ = 64 ng/mL)^[1].
IGM-8444 (24 h) potently induces cytotoxicity in Colo205 colorectal cancer cells (IC₅₀ = 1.1 ng/mL) and H-EMC-SS chondrosarcoma cells (IC₅₀ = 0.32 ng/mL)^[1].
IGM-8444 (1 μg/mL; 0.5-6 h) rapidly and potently activates caspase-3/7, caspase-8, and caspase-9 in Colo205 colorectal cancer cells and H-EMC-SS chondrosarcoma cells^[1].
Treatment with IGM-8444 (1 μg/mL; 1-6 h) for 6 h induces early apoptosis in 23% of Colo205 colorectal cancer cells and 15% of H-EMC-SS chondrosarcoma cells^[1].
IGM-8444 (72 h) exhibits synergistic cytotoxicity with chemotherapeutic agents and ABT-199 (HY-15531) in HCT15 colorectal cancer cells, NCI-H2228 non-small cell lung cancer cells, and MV-411 acute myeloid leukemia cells, with a maximum Bliss score ranging from 16.8 to 53.4^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Apoptosis Analysis^[1]

Cell Line:

Colo205 colorectal cancer cells, H-EMC-SS chondrosarcoma cells
Concentration:

1 μg/mL
Incubation Time:

1, 3, 6 h
Result:

Induced early apoptosis in 23% of Colo205 cells and 15% of H-EMC-SS cells after 6 hours of treatment.
Showed significantly more early apoptosis induction than the corresponding anti-DR5 IgG (4% and 2% early apoptotic cells for Colo205 and H-EMC-SS, respectively), which was similar to isotype controls.

In Vivo

IGM-8444 (0.3-10 mg/kg; intravenous injection; single dose or once every other day; 11 doses total) dose-dependently inhibits the growth of Colo205 colorectal tumors in mice^[1].
IGM-8444 (5 mg/kg; intravenous injection; once every 2 days; 11 doses total) induces 101% tumor growth inhibition (TGI) in NCI-H2122 non-small cell lung cancer xenografts and extends the median event-free survival by 40 days^[1].
IGM-8444 (0.3-10 mg/kg; intravenous injection; once every other day) induces potent and sustained tumor regression in the GXF251 gastric cancer PDX model^[1].
IGM-8444 (5 mg/kg; intravenous injection; once every other day; 7 doses total) , in combination with irinotecan (HY-16562), 5-FU (HY-90006) or Paclitaxel (HY-B0015), enhances the antitumor efficacy in the Colo205 colorectal cancer xenograft model^[1].
IGM-8444 (5 mg/kg; intravenous injection; once every two days; 11 doses total) combined with ABT-199 induces 102% TGI and prolongs survival in mice bearing DOHH-2 non-Hodgkin's lymphoma xenografts^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Crl:NU (Ncr)-Foxn1nu (female, 8-12-weeks-old, subcutaneous implantation of 2×10⁶ Colo205 cells)^[1]
Dosage:

0.3, 1, 3 and 10 mg/kg (tumor growth inhibition); 0.3, 1, 3, 10 and 20 mg/kg (biomarker analysis)
Administration:

i.v.; every other day; 11 doses (tumor growth inhibition); i.v.; single dose (biomarker analysis)
Result:

Induced 23%, 29%, 75%, and 84% tumor growth inhibition (TGI) on day 22 at doses of 0.3, 1, 3, and 10 mg/kg, respectively.
Increased serum M30 up to 10-fold and M65 up to 5-fold in a dose-dependent manner 24 hours after single doses.

Animal Model:

Crl:NU (Ncr)-Foxn1nu (female, 8-12-weeks-old, subcutaneous implantation of 10⁷ NCI-H2122 cells)^[1]
Dosage:

5 mg/kg
Administration:

i.v.; every other day; 11 doses (tumor growth and survival); i.v.; single dose (biomarker analysis)
Result:

Induced 101% TGI on day 26, with 5/10 animals achieving a partial response (PR).
Extended median event-free survival by 40 days compared with vehicle.
Significantly elevated cleaved caspase-3 (CC3) staining in tumor tissue 24 hours after a single dose.

Animal Model:

NMRI nude (female, 5-7-weeks-old, subcutaneous implantation of 3-4 mm GXF251 PDX tumor fragments)^[1]
Dosage:

0.3, 1, 3 and 10 mg/kg (dose-dependent study); 5 mg/kg (fixed dose, different tumor sizes)
Administration:

i.v.; every other day; 7 doses (fixed dose); i.v.; every other day (dose-dependent study); i.v.; weekly (weekly dosing study)
Result:

Induced 112% TGI on day 46 at 5 mg/kg every other day for 7 doses, with 8/10 complete responses (CR), 2/10 partial responses (PR), 7/10 event-free animals, and 6/10 tumor-free survivors (TFS) at day 99.
Elevated serum M30 10-fold and M65 6-fold 24 hours post-treatment.
Induced 30%, 55%, 101%, and 99% TGI on day 59 at doses of 0.3, 1, 3, and 10 mg/kg every other day, respectively, with 2/7 tumor-free animals in the 10 mg/kg group at day 100.
Induced 58% and 102% TGI on day 28 with weekly dosing of 1 and 10 mg/kg, respectively.
Induced 112%, 103%, and 101% TGI on day 32 when dosed into tumors with initial volumes of 100, 300, or 500 mm³, respectively.

Animal Model:

Crl:NU (Ncr)-Foxn1nu (female, 8-12-weeks-old, subcutaneous implantation of 2×10⁶ Colo205 cells)^[1]
Dosage:

5 mg/kg (single agent); 5 mg/kg + 100 mg/kg irinotecan; 5 mg/kg + 100 mg/kg 5-FU; 5 mg/kg + 25 mg/kg paclitaxel
Administration:

i.v.; every other day; 7 doses (IGM-8444); i.p.; weekly; 3 weeks (Irinotecan, 5-FU); i.v.; every other day; 5 doses (Paclitaxel)
Result:

Induced 70%-76% TGI as a single agent at 5 mg/kg.
Combination with Irinotecan induced 103% TGI with 2/10 PRs and extended median event-free survival by 42 days compared with vehicle.
Combination with 5-FU induced 104% TGI with 3/10 PRs and 1/10 CR/TFS, without additional toxicity compared with 5-FU alone.
Combination with paclitaxel increased CR rate from 30% (Paclitaxel alone) to 100%, with 8/10 animals tumor-free at day 100 compared with 2/10 in the Paclitaxel-only group.

Animal Model:

Fox Chase SCID, CB17/Icr-Prkdcscid/IcrIcoCrl (female, 9-weeks-old, subcutaneous implantation of 10⁷ DOHH-2 cells)^[1]
Dosage:

5 mg/kg (single agent); 5 mg/kg + 100 mg/kg ABT-199
Administration:

i.v.; every other day; 11 doses (IGM-8444); p.o.; daily; 21 days (ABT-199)
Result:

Induced 45% TGI as a single agent at 5 mg/kg.
Combination with ABT-199 induced 102% TGI with 3/10 PRs and 2/10 CRs.
Significantly extended median event-free survival compared with vehicle or ABT-199 alone.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Gene ID

8795 [NCBI]

Accession

O14763

Conjugated

Unconjugated

Reconsititution

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

Format

IgM-kappa_Jchain

Anwendung

ELISA, FACS, Functional assay

Verified Bioactivity

Immobilized TRAIL R2/TNFRSF10B Protein, Human (HY-P72779) can bind Aplitabart. The EC₅₀ for this effect is 201.8 ng/mL.

Chemical Information

CAS. Nr. 2796349-94-3
Appearance Liquid
Molecular Weight 871.57 kDa
Color Colorless to off-white
SMILES

[Aplitabart]
Synonyms

IGM-8444
Versand

Shipping with dry ice.
Formulation

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

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (268 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Inhibitory Antibodies User Guide (603 KB)

Verweise

[1]. Wang BT, et al. Multimeric Anti-DR5 IgM Agonist Antibody IGM-8444 Is a Potent Inducer of Cancer Cell Apoptosis and Synergizes with Chemotherapy and BCL-2 Inhibitor ABT-199. Mol Cancer Ther. 2021;20(12):2483-2494. [Content Brief]

[2]. Wang BT, et al. The Anti-Tumor Activity of Igm-8444, an Agonistic Death Receptor 5 (DR5) IgM Antibody, Is Sensitized in Combination with Chemotherapy and Bcl-2 Inhibitors in NHL and AML. Blood. 2020 Nov 5;136:43-4.

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Aplitabart

Cytotoxicity LDH Assay Kit

PBS Buffer (1×)

DPBS Buffer (1×)

Alle TNF Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

Aplitabart Related Classifications

HY-P990901 Related Classifications