PTC-028 | CAS#1782970-28-8 | antitumor agent

MedKoo Cat#: 584452 | Name: PTC-028

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Description:

WARNING: This product is for research use only, not for human or veterinary use.

PTC-028 is an orally bioavailable compound that decreases BMI-1 levels by posttranslational modification. In vivo, orally administered PTC-028, as a single agent, exhibits significant antitumor activity comparable with the standard cisplatin/paclitaxel therapy in an orthotopic mouse model of ovarian cancer.

Chemical Structure

PTC-028

CAS#1782970-28-8

Theoretical Analysis

MedKoo Cat#: 584452

Name: PTC-028

CAS#: 1782970-28-8

Chemical Formula: C19H12F5N5

Exact Mass: 405.1013

Molecular Weight: 405.33

Elemental Analysis: C, 56.30; H, 2.98; F, 23.44; N, 17.28

Price and Availability

Size	Price	Availability	Quantity
5mg	USD 330.00
25mg	USD 740.00
1g	USD 3,250.00
2g	USD 5,850.00
5g	USD 9,850.00

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Related CAS #

No Data

Synonym

PTC-028; PTC028; PTC 028

IUPAC/Chemical Name

2-Pyrazinamine, 6-(5,6-difluoro-2-methyl-1H-benzimidazol-1-yl)-N-[4-(trifluoromethyl)phenyl]-

InChi Key

JEZGPBWIZWPDHP-UHFFFAOYSA-N

InChi Code

InChI=1S/C19H12F5N5/c1-10-26-15-6-13(20)14(21)7-16(15)29(10)18-9-25-8-17(28-18)27-12-4-2-11(3-5-12)19(22,23)24/h2-9H,1H3,(H,27,28)

SMILES Code

FC(C1=CC=C(NC2=NC(N3C4=CC(F)=C(F)C=C4N=C3C)=CN=C2)C=C1)(F)F

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO and ethanol

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

PTC-028 effectively inhibits the proliferation of ovarian cancer cells OVCAR-4 and OV-90, with IC50 values of approximately 0.1 µM for both. PTC-028 induces BMI1 degradation and concentration-dependent apoptosis in these cells. PTC-028 disrupts microtubule polymerization and triggers G2/M cell cycle arrest in MDS-L myelodysplastic syndrome cells. PTC-028 effectively reduces tumor growth in an OV-90 orthotopic mouse model of ovarian cancer.

In vitro activity:

In a myelodysplastic syndrome (MDS) model, PTC-028 suppressed growth and induced apoptosis in MDS cell lines by synergizing with hypomethylating agents, such as decitabine and azacitidine. PTC-028 treatment induced G2/M arrest followed by apoptotic cell death. Reference: Cancer Sci. 2020 Dec;111(12):4336-4347. https://pubmed.ncbi.nlm.nih.gov/33037737/

In vivo activity:

When administered to mice xenografted with medulloblastoma tumors, PTC-028 significant reduced tumor burden in both local and metastatic compartments and subsequent increased survival without neurotoxicity. Reference: Oncogene. 2019 Mar;38(10):1702-1716. https://pubmed.ncbi.nlm.nih.gov/30348991/

	Solvent	mg/mL	mM
Solubility
	DMSO	81.0	199.84
	Ethanol	17.0	41.94

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 405.33 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Zhong C, Kayamori K, Koide S, Shinoda D, Oshima M, Nakajima-Takagi Y, Nagai Y, Mimura N, Sakaida E, Yamazaki S, Iwano S, Miyawaki A, Ito R, Tohyama K, Yamaguchi K, Furukawa Y, Lennox W, Sheedy J, Weetall M, Iwama A. Efficacy of the novel tubulin polymerization inhibitor PTC-028 for myelodysplastic syndrome. Cancer Sci. 2020 Dec;111(12):4336-4347. doi: 10.1111/cas.14684. Epub 2020 Nov 2. PMID: 33037737; PMCID: PMC7734154. 2. Bolomsky A, Muller J, Stangelberger K, Lejeune M, Duray E, Breid H, Vrancken L, Pfeiffer C, Hübl W, Willheim M, Weetall M, Branstrom A, Zojer N, Caers J, Ludwig H. The anti-mitotic agents PTC-028 and PTC596 display potent activity in pre-clinical models of multiple myeloma but challenge the role of BMI-1 as an essential tumour gene. Br J Haematol. 2020 Sep;190(6):877-890. doi: 10.1111/bjh.16595. Epub 2020 Mar 30. PMID: 32232850. 3. Bakhshinyan D, Venugopal C, Adile AA, Garg N, Manoranjan B, Hallett R, Wang X, Mahendram S, Vora P, Vijayakumar T, Subapanditha M, Singh M, Kameda-Smith MM, Qazi M, McFarlane N, Mann A, Ajani OA, Yarascavitch B, Ramaswamy V, Farooq H, Morrissy S, Cao L, Sydorenko N, Baiazitov R, Du W, Sheedy J, Weetall M, Moon YC, Lee CS, Kwiecien JM, Delaney KH, Doble B, Cho YJ, Mitra S, Kaplan D, Taylor MD, Davis TW, Singh SK. BMI1 is a therapeutic target in recurrent medulloblastoma. Oncogene. 2019 Mar;38(10):1702-1716. doi: 10.1038/s41388-018-0549-9. Epub 2018 Oct 22. PMID: 30348991. 4. Buechel M, Dey A, Dwivedi SKD, Crim A, Ding K, Zhang R, Mukherjee P, Moore KN, Cao L, Branstrom A, Weetall M, Baird J, Bhattacharya R. Inhibition of BMI1, a Therapeutic Approach in Endometrial Cancer. Mol Cancer Ther. 2018 Oct;17(10):2136-2143. doi: 10.1158/1535-7163.MCT-17-1192. Epub 2018 Jul 19. PMID: 30026381; PMCID: PMC7285980.

In vitro protocol:

In vivo protocol:

1. Bakhshinyan D, Venugopal C, Adile AA, Garg N, Manoranjan B, Hallett R, Wang X, Mahendram S, Vora P, Vijayakumar T, Subapanditha M, Singh M, Kameda-Smith MM, Qazi M, McFarlane N, Mann A, Ajani OA, Yarascavitch B, Ramaswamy V, Farooq H, Morrissy S, Cao L, Sydorenko N, Baiazitov R, Du W, Sheedy J, Weetall M, Moon YC, Lee CS, Kwiecien JM, Delaney KH, Doble B, Cho YJ, Mitra S, Kaplan D, Taylor MD, Davis TW, Singh SK. BMI1 is a therapeutic target in recurrent medulloblastoma. Oncogene. 2019 Mar;38(10):1702-1716. doi: 10.1038/s41388-018-0549-9. Epub 2018 Oct 22. PMID: 30348991. 2. Buechel M, Dey A, Dwivedi SKD, Crim A, Ding K, Zhang R, Mukherjee P, Moore KN, Cao L, Branstrom A, Weetall M, Baird J, Bhattacharya R. Inhibition of BMI1, a Therapeutic Approach in Endometrial Cancer. Mol Cancer Ther. 2018 Oct;17(10):2136-2143. doi: 10.1158/1535-7163.MCT-17-1192. Epub 2018 Jul 19. PMID: 30026381; PMCID: PMC7285980.

1: Polmear J, Hailes L, Olshansky M, Rischmueller M, L'Estrange-Stranieri E, Fletcher AL, Hibbs ML, Bryant VL, Good-Jacobson KL. Targeting BMI-1 to deplete antibody-secreting cells in autoimmunity. Clin Transl Immunology. 2023 Oct 4;12(10):e1470. doi: 10.1002/cti2.1470. PMID: 37799772; PMCID: PMC10550498. 2: Shields CE, Potlapalli S, Cuya-Smith SM, Chappell SK, Chen D, Martinez D, Pogoriler J, Rathi KS, Patel SA, Oristian KM, Linardic CM, Maris JM, Haynes KA, Schnepp RW. Epigenetic regulator BMI1 promotes alveolar rhabdomyosarcoma proliferation and constitutes a novel therapeutic target. Mol Oncol. 2021 Aug;15(8):2156-2171. doi: 10.1002/1878-0261.12914. Epub 2021 Mar 27. PMID: 33523558; PMCID: PMC8333775. 3: Balakrishnan I, Danis E, Pierce A, Madhavan K, Wang D, Dahl N, Sanford B, Birks DK, Davidson N, Metselaar DS, Meel MH, Lemma R, Donson A, Vijmasi T, Katagi H, Sola I, Fosmire S, Alimova I, Steiner J, Gilani A, Hulleman E, Serkova NJ, Hashizume R, Hawkins C, Carcaboso AM, Gupta N, Monje M, Jabado N, Jones K, Foreman N, Green A, Vibhakar R, Venkataraman S. Senescence Induced by BMI1 Inhibition Is a Therapeutic Vulnerability in H3K27M-Mutant DIPG. Cell Rep. 2020 Oct 20;33(3):108286. doi: 10.1016/j.celrep.2020.108286. PMID: 33086074; PMCID: PMC7574900. 4: Zhong C, Kayamori K, Koide S, Shinoda D, Oshima M, Nakajima-Takagi Y, Nagai Y, Mimura N, Sakaida E, Yamazaki S, Iwano S, Miyawaki A, Ito R, Tohyama K, Yamaguchi K, Furukawa Y, Lennox W, Sheedy J, Weetall M, Iwama A. Efficacy of the novel tubulin polymerization inhibitor PTC-028 for myelodysplastic syndrome. Cancer Sci. 2020 Dec;111(12):4336-4347. doi: 10.1111/cas.14684. Epub 2020 Nov 2. PMID: 33037737; PMCID: PMC7734154. 5: Bolomsky A, Muller J, Stangelberger K, Lejeune M, Duray E, Breid H, Vrancken L, Pfeiffer C, Hübl W, Willheim M, Weetall M, Branstrom A, Zojer N, Caers J, Ludwig H. The anti-mitotic agents PTC-028 and PTC596 display potent activity in pre-clinical models of multiple myeloma but challenge the role of BMI-1 as an essential tumour gene. Br J Haematol. 2020 Sep;190(6):877-890. doi: 10.1111/bjh.16595. Epub 2020 Mar 30. PMID: 32232850. 6: Bakhshinyan D, Venugopal C, Adile AA, Garg N, Manoranjan B, Hallett R, Wang X, Mahendram S, Vora P, Vijayakumar T, Subapanditha M, Singh M, Kameda-Smith MM, Qazi M, McFarlane N, Mann A, Ajani OA, Yarascavitch B, Ramaswamy V, Farooq H, Morrissy S, Cao L, Sydorenko N, Baiazitov R, Du W, Sheedy J, Weetall M, Moon YC, Lee CS, Kwiecien JM, Delaney KH, Doble B, Cho YJ, Mitra S, Kaplan D, Taylor MD, Davis TW, Singh SK. BMI1 is a therapeutic target in recurrent medulloblastoma. Oncogene. 2019 Mar;38(10):1702-1716. doi: 10.1038/s41388-018-0549-9. Epub 2018 Oct 22. PMID: 30348991. 7: Buechel M, Dey A, Dwivedi SKD, Crim A, Ding K, Zhang R, Mukherjee P, Moore KN, Cao L, Branstrom A, Weetall M, Baird J, Bhattacharya R. Inhibition of BMI1, a Therapeutic Approach in Endometrial Cancer. Mol Cancer Ther. 2018 Oct;17(10):2136-2143. doi: 10.1158/1535-7163.MCT-17-1192. Epub 2018 Jul 19. PMID: 30026381; PMCID: PMC7285980. 8: Dey A, Xiong X, Crim A, Dwivedi SKD, Mustafi SB, Mukherjee P, Cao L, Sydorenko N, Baiazitov R, Moon YC, Dumble M, Davis T, Bhattacharya R. Evaluating the Mechanism and Therapeutic Potential of PTC-028, a Novel Inhibitor of BMI-1 Function in Ovarian Cancer. Mol Cancer Ther. 2018 Jan;17(1):39-49. doi: 10.1158/1535-7163.MCT-17-0574. Epub 2017 Nov 20. PMID: 29158468; PMCID: PMC5752598.