2. Immunology/Inflammation Apoptosis
  3. PSMA Apoptosis
  4. Pelgifatamab

Pelgifatamab  (Synonyms: BAY-2315497; PSMA-TTC)

Cat. No.: HY-P9992 Purity: 99.884%
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Peligifatamab is a PSMA-targeted α-radioimmunoconjugate with an EC50 of 1.2 nM against human targets. Peligifatamab induces DNA damage, DNA double-strand breaks, cell cycle arrest and apoptosis (Apoptosis) in PSMA-positive prostate cancer cells. Peligifatamab reduces cell viability in a manner dependent on cellular PSMA expression levels. Peligifatamab inhibits tumor growth and tumor-induced abnormal bone growth in prostate cancer bone metastasis models. Peligifatamab exhibits antitumor efficacy in subcutaneous prostate cancer models and xenograft models. Peligifatamab can be used for the research of metastatic castration-resistant prostate cancer.

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CAS No. : 2414550-93-7

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Description

Peligifatamab is a PSMA-targeted α-radioimmunoconjugate with an EC50 of 1.2 nM against human targets. Peligifatamab induces DNA damage, DNA double-strand breaks, cell cycle arrest and apoptosis (Apoptosis) in PSMA-positive prostate cancer cells. Peligifatamab reduces cell viability in a manner dependent on cellular PSMA expression levels. Peligifatamab inhibits tumor growth and tumor-induced abnormal bone growth in prostate cancer bone metastasis models. Peligifatamab exhibits antitumor efficacy in subcutaneous prostate cancer models and xenograft models. Peligifatamab can be used for the research of metastatic castration-resistant prostate cancer[1].

Isotype

Human IgG1 kappa
Recommend Isotype Controls
Species Reactivity

Human
IC50 & Target

FOLH1/PSMA
In Vivo

Peligifatamab (75-500 kBq/kg; i.v.; single dose; weekly; biweekly) induces dose-dependent antitumor efficacy in the LNCaP subcutaneous xenograft model[1].
Peligifatamab (100-500 kBq/kg; i.v.; single dose) exhibits potent antitumor efficacy in androgen-independent and castration-resistant subcutaneous prostate cancer xenografts, with a T/C ratio as low as 0.09 at a single dose of 500 kBq/kg in MDA-PCa-2b xenografts[1].
Peligifatamab (75-500 kBq/kg; 4×75 kBq/kg; 4×125 kBq/kg; 2×150 kBq/kg; 2×250 kBq/kg; i.v.; single dose; weekly; biweekly) induces potent antitumor efficacy in xenografts of prostate cancer, with a T/C ratio as low as 0.01 in ST1273 xenografts when a single dose of 500 kBq/kg is administered[1].
Peligifatamab (100-200 kBq/kg; i.v.; single dose) potently inhibits tumor growth and tumor-induced bone tissue changes in an intratibial prostate cancer bone metastasis model, with a single dose of 100 kBq/kg resulting in a T/C ratio of 0.03[1].
Peligifatamab (500 kBq/kg; total antibody 0.14-5 mg/kg; i.v.; single dose) maintains potent antitumor efficacy in the 22Rv1 xenograft model when the total antibody dose ranges from 0.14 to 1.5 mg/kg, whereas the efficacy decreases at a total antibody dose of 5 mg/kg[1].

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

Animal Model: CB17-Scid (male)[1]
Dosage: 75 kBq/kg ; 150 kBq/kg ; 300 kBq/kg; 4 × 75 kBq/kg; 2 × 150 kBq
Administration: i.v.; single dose; weekly for 4 doses; biweekly for 2 doses
Result: Achieved T/C ratios of 0.51, 0.42, and 0.31 with single doses of 75, 150, and 300 kBq/kg, respectively.
Resulted in 7 of 10 mice showing partial response or stable disease with 300 kBq/kg single dose.
Achieved T/C ratios of 0.07 and 0.12 with fractionated doses of 4 × 75 kBq/kg and 2 × 150 kBq/kg, respectively.
Animal Model: athymic nude (male); NMRI Nude (male)[1]
Dosage: 100 kBq/kg (0.14 mg/kg total antibody); 250 kBq/kg (0.14 mg/kg total antibody); 500 kBq/kg (0.14 mg/kg total antibody)
Administration: i.v.; single dose
Result: Achieved T/C ratios of 0.33, 0.18, and 0.09 with single doses of 100, 250, and 500 kBq/kg in MDA-PCa-2b xenografts, respectively.
Achieved T/C ratios of 0.54, 0.37, and 0.19 with single doses of 100, 250, and 500 kBq/kg in 22Rv1 xenografts, respectively.
Achieved T/C ratios of 0.27, 0.47, and 0.15 with single doses of 100, 250, and 500 kBq/kg in C4-2 xenografts, respectively.
Induced statistically significant tumor growth inhibition at ≥250 kBq/kg in MDA-PCa-2b and 22Rv1 models, and starting at 100 kBq/kg in the C4-2 model.
Animal Model: NMRI nude (female); CB17-Scid (male)[1]
Dosage: 125 kBq/kg (0.14 mg/kg total antibody); 250 kBq/kg (0.14 mg/kg total antibody); 500 kBq/kg (0.14 mg/kg total antibody); 4 × 125 kBq/kg (0.14 mg/kg total antibody per dose); 2 × 250 kBq/kg (0.14 mg/kg total antibody per dose); 75 kBq/kg (0.14 mg/kg total antibody); 150 kBq/kg (0.14 mg/kg total antibody); 300 kBq/kg (0.14 mg/kg total antibody); 4 × 75 kBq/kg (0.14 mg/kg total antibody per dose); 2 × 150 kBq/kg (0.14 mg/kg total antibody per dose)
Administration: i.v.; single dose; weekly for 4 doses; biweekly for 2 doses
Result: Achieved T/C ratios of 0.3, 0.05, and 0.01 with single doses of 125, 250, and 500 kBq/kg in ST1273 xenografts, respectively.
Resulted in 5 partial responses and 4 complete responses out of 10 mice with 500 kBq/kg single dose in ST1273 xenografts.
Reduced serum PSA levels effectively with 250 and 500 kBq/kg single doses in ST1273 xenografts.
Achieved T/C ratios of 0.13 and 0.04 with fractionated doses of 4 × 125 kBq/kg and 2 × 250 kBq/kg in ST1273 xenografts, respectively.
Achieved T/C ratios of 0.39, 0.28, and 0.07 with single doses of 75, 150, and 300 kBq/kg in KUCaP-1 xenografts, respectively.
Resulted in 2 stable disease and 6 partial responses out of 10 mice with 300 kBq/kg single dose in KUCaP-1 xenografts.
Achieved T/C ratios of 0.24 and 0.25 with fractionated doses of 4 × 75 kBq/kg and 2 × 150 kBq/kg in KUCaP-1 xenografts, respectively.
Achieved T/C ratios of 0.58 and 0.27 with single doses of 150 and 300 kBq/kg in LuCaP 86.2 xenografts, respectively.
Resulted in 5 stable disease, 1 partial response, and 1 complete response out of 10 mice with 300 kBq/kg single dose in LuCaP 86.2 xenografts.
Animal Model: NOD.scid (male)[1]
Dosage: 100 kBq/kg (0.14 mg/kg total antibody); 200 kBq/kg (0.14 mg/kg total antibody)
Administration: i.v.; single dose
Result: Reduced LNCaP-luc tumor burden in bone with T/C ratios of 0.03 and 0.14 based on bioluminescence with single doses of 100 and 200 kBq/kg, respectively.
Lowered serum PSA levels with single doses of 100 and 200 kBq/kg.
Significantly inhibited the total area of tumor-induced bone changes compared to vehicle controls with single doses of 100 and 200 kBq/kg.
Animal Model: NMRI Nude (male)[1]
Dosage: 500 kBq/kg (0.14 mg/kg total antibody); 500 kBq/kg (0.75 mg/kg total antibody); 500 kBq/kg (1.5 mg/kg total antibody); 500 kBq/kg (5 mg/kg total antibody)
Administration: i.v.; single dose
Result: Achieved T/C ratios of 0.13-0.31 with single 500 kBq/kg doses at total antibody doses of 0.14, 0.75, and 1.5 mg/kg.
Resulted in reduced efficacy with a T/C ratio of 0.84 with single 500 kBq/kg dose at 5 mg/kg total antibody dose.
Gene ID

2346  [NCBI]

Accession
Application

ELISA, FACS, Functional assay
Conjugated

Unconjugated
Reconsititution

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

146.24 kDa

CAS No.
Appearance

Liquid

Color

Colorless to light yellow

SMILES

[Pelgifatamab]
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
  • Human IgG1 kappa
Biological Activity
  • Immobilized PSMA Protein, Human (HEK293, N-His, HY-P70548A) can bind Pelgifatamab. The EC50 for this effect is 107.5 ng/mL.
Purity & Documentation
References
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Pelgifatamab Related Classifications

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Help & FAQs
  • 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:

Pelgifatamab2414550-93-7BAY-2315497 PSMA-TTCBAY2315497BAY 2315497PSMAApoptosisProstate-specific membrane antigenPSMA-targeted α-radioimmunoconjugatemetastatic castration-resistant prostate cancerNMRI Nudemice
Inhibitorinhibitorinhibit

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