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MedKoo Cat#: 407928 | Name: BAY-8002
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Description:

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

BAY-8002 is a Monocarboxylate Transporter 1 Inhibitor. The lactate transporter SLC16A1/MCT1 plays a central role in tumor cell energy homeostasis. BAY-8002, which potently suppress bidirectional lactate transport. BAY-8002 significantly increased intratumor lactate levels and transiently modulated pyruvate levels.

Chemical Structure

BAY-8002
BAY-8002
CAS#724440-27-1

Theoretical Analysis

MedKoo Cat#: 407928

Name: BAY-8002

CAS#: 724440-27-1

Chemical Formula: C20H14ClNO5S

Exact Mass: 415.0281

Molecular Weight: 415.84

Elemental Analysis: C, 57.77; H, 3.39; Cl, 8.52; N, 3.37; O, 19.24; S, 7.71

Price and Availability

Size Price Availability Quantity
50mg USD 450.00 2 Weeks
100mg USD 750.00 2 Weeks
200mg USD 1,250.00 2 Weeks
500mg USD 1,950.00 2 Weeks
1g USD 2,950.00 2 Weeks
2g USD 5,250.00 2 Weeks
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Related CAS #
No Data
Synonym
BAY-8002; BAY 8002; BAY8002;
IUPAC/Chemical Name
2-(2-chloro-5-(phenylsulfonyl)benzamido)benzoic acid
InChi Key
CLAUJSRBKSRTGQ-UHFFFAOYSA-N
InChi Code
InChI=1S/C20H14ClNO5S/c21-17-11-10-14(28(26,27)13-6-2-1-3-7-13)12-16(17)19(23)22-18-9-5-4-8-15(18)20(24)25/h1-12H,(H,22,23)(H,24,25)
SMILES Code
O=C(O)C1=CC=CC=C1NC(C2=CC(S(=O)(C3=CC=CC=C3)=O)=CC=C2Cl)=O
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
Shelf Life
>3 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:
BAY-8002 is an inhibitor of monocarboxylate transporter 1 (MCT1) with an IC50 of 85 nM.
In vitro activity:
Because MCT1 facilitates bidirectional lactate transport, the effect of BAY-8002 on lactate extrusion was evaluated. BAY-8002 inhibited the accumulation of lactate in the cell supernatant (Fig. 1E) and decreased the ECAR (Fig. 1F). In both assays, only 60% efficacy in blocking the export of lactate was observed. This effect was observed in different cell lines and may be due to the free diffusion at lower pH of the undissociated lactic acid across the cell membrane. The inhibition of lactate transport resulted in efficient proliferation inhibition of MCT1-expressing Raji and Daudi Burkitt lymphoma cells (Fig. 1B and G). Reference: Mol Cancer Ther. 2018 Nov;17(11):2285-2296. https://mct.aacrjournals.org/content/17/11/2285.long
In vivo activity:
In order to investigate antitumor efficacy, Raji tumor–bearing mice were treated twice daily per os with 80 and 160 mg/kg BAY-8002. This treatment schedules allowed for compound plasma levels that ensured continuous target inhibition (Fig. 4D). The treatment was very well tolerated, and no significant body weight loss was observed (Fig. 4B and C). BAY-8002 showed significant inhibition of tumor growth; however, no tumor regression was observed (Fig. 4B). Reference: Mol Cancer Ther. 2018 Nov;17(11):2285-2296. https://mct.aacrjournals.org/content/17/11/2285.long
Solvent mg/mL mM
Solubility
DMSO 83.2 200.05
Ethanol 28.0 67.33
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 415.84 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.

Recalculate based on batch purity %
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. Quanz M, Bender E, Kopitz C, Grünewald S, Schlicker A, Schwede W, Eheim A, Toschi L, Neuhaus R, Richter C, Toedling J, Merz C, Lesche R, Kamburov A, Siebeneicher H, Bauser M, Hägebarth A. Preclinical Efficacy of the Novel Monocarboxylate Transporter 1 Inhibitor BAY-8002 and Associated Markers of Resistance. Mol Cancer Ther. 2018 Nov;17(11):2285-2296. doi: 10.1158/1535-7163.MCT-17-1253. Epub 2018 Aug 16. PMID: 30115664.
In vitro protocol:
1. Quanz M, Bender E, Kopitz C, Grünewald S, Schlicker A, Schwede W, Eheim A, Toschi L, Neuhaus R, Richter C, Toedling J, Merz C, Lesche R, Kamburov A, Siebeneicher H, Bauser M, Hägebarth A. Preclinical Efficacy of the Novel Monocarboxylate Transporter 1 Inhibitor BAY-8002 and Associated Markers of Resistance. Mol Cancer Ther. 2018 Nov;17(11):2285-2296. doi: 10.1158/1535-7163.MCT-17-1253. Epub 2018 Aug 16. PMID: 30115664.
In vivo protocol:
1. Quanz M, Bender E, Kopitz C, Grünewald S, Schlicker A, Schwede W, Eheim A, Toschi L, Neuhaus R, Richter C, Toedling J, Merz C, Lesche R, Kamburov A, Siebeneicher H, Bauser M, Hägebarth A. Preclinical Efficacy of the Novel Monocarboxylate Transporter 1 Inhibitor BAY-8002 and Associated Markers of Resistance. Mol Cancer Ther. 2018 Nov;17(11):2285-2296. doi: 10.1158/1535-7163.MCT-17-1253. Epub 2018 Aug 16. PMID: 30115664.
1: Quanz M, Bender E, Kopitz C, Grünewald S, Schlicker A, Schwede W, Eheim A, Toschi L, Neuhaus R, Richter C, Toedling J, Merz C, Lesche R, Kamburov A, Siebeneicher H, Bauser M, Haegebarth A. Preclinical Efficacy of the Novel Monocarboxylate Transporter 1 Inhibitor BAY-8002 and Associated Markers of Resistance. Mol Cancer Ther. 2018 Aug 16. pii: molcanther.1253.2017. doi: 10.1158/1535-7163.MCT-17-1253. [Epub ahead of print] PubMed PMID: 30115664.