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| Targets |
Carba1 targets two distinct molecular entities: (1) tubulin, where it occupies the colchicine‑binding site, acting as a microtubule‑destabilizing agent that promotes catastrophes; (2) nicotinamide phosphoribosyltransferase (NAMPT), the rate‑limiting enzyme in the NAD salvage pathway, which it activates to boost NAD biosynthesis. By binding to the colchicine site, Carba1 reduces the required taxane dose and potentiates paclitaxel binding to microtubule ends, enhancing antitumor synergy without increasing toxicity.
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| ln Vitro |
Carba1 (12 μM; 72 h) synergistically inhibited the viability of HeLa cells with Paclitaxel, Docetaxel, nab-Paclitaxel and Epipothilone-B, reducing their GI50 values by 2.6, 3.8, 1.8 and 4.4 times [1]. Carba1 (1-20 μM; 60 mins) enhanced NAMPT activity in HeLa cells [1]. Carba1 (12 μM; 72 h) protected adult mouse DRG neurons from axonal degeneration induced by Paclitaxel, Cisplatin and Bortezomib, reducing the degeneration index [1]. Carba1 (1-10 μM; 24 h) counteracted Cisplatin-induced neurotoxicity and myelination disorder in rat DRG neurons [1]. Carba1 (12 μM, 2 h) regulates HeLa cell metabolism, increases lactate, glutamate, ATP and GTP levels, decreases NAD+ levels, and enhances glycolysis and glutamine breakdown [1].
In vitro, Carba1 (12 microM; 72 h) synergizes with paclitaxel, docetaxel, nab‑paclitaxel and epothilone‑B to inhibit HeLa cell viability, reducing GI₅0 values by 2.6‑ to 4.4‑fold. It (1‑20 microM; 60 min) enhances NAMPT activity in HeLa cells, and (12 microM; 72 h) protects mouse DRG neurons from paclitaxel‑, cisplatin‑ and bortezomib‑induced axonal degeneration, reducing the degeneration index. It also counteracts cisplatin‑induced neurotoxicity and demyelination in rat DRG neurons (1‑10 microM; 24 h). |
| ln Vivo |
Carba1 (50 mg/kg; intraperitoneal injection; days 0, 1, 2, 4, 7 and 9) prevented abnormal pain and neurodegeneration in a paclitaxel-induced neuropathic injury model [1]. Carba1 (60 mg/kg; intravenous injection; every 2 days for 10 days) did not promote tumor growth or inhibit the antitumor activity of paclitaxel in a tumor growth model. [1]
In vivo, Carba1 (50 mg/kg; i.p. on days 0,1,2,4,7,9) fully prevents tactile allodynia and neurodegeneration in a paclitaxel‑induced rat CIPN model, reduces serum neurofilament light chain (NfL) levels, and maintains intraepidermal nerve fiber (IENF) density. Carba1 (60 mg/kg; i.v. every 2 days for 10 days) does not promote tumor growth nor inhibit paclitaxel's antitumor efficacy in a xenograft tumor model. In xenografted mice, Carba1 synergizes with sub‑therapeutic paclitaxel to kill cancer cells. |
| Enzyme Assay |
The non‑cellular tubulin binding assay uses [3H]‑colchicine competition: purified tubulin is incubated with 50 nM [3H]‑colchicine and increasing concentrations of unlabeled Carba1 (e.g., 100 microM) at 37 degC. Bound radioactivity is separated by filtration or charcoal adsorption, and IC₅0 is calculated. For NAMPT, a triply coupled enzymatic assay measures NAD production from nicotinamide and phosphoribosyl pyrophosphate via spectrophotometric detection. Binding is confirmed by AS‑MS after size‑exclusion chromatography (10 microM Carba1 with 3 microM NAMPT).
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| Cell Assay |
Cell‑based assays use HeLa cells (viability synergy), primary mouse DRG neurons (axonal degeneration), rat DRG neurons (myelination), or Schwann cells (MPB staining). Cells are treated with Carba1 (0‑20 microM; 24‑72 h) alone or with chemotherapeutics. Viability is assessed by CellTiter‑Glo or MTT. Neuroprotection endpoints include degeneration index, myelin basic protein (MBP) staining, and quantification of NAD+/ATP/GTP levels. NAMPT activation is measured by cellular NAD levels after Carba1 exposure.
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| Animal Protocol |
Animal/Disease Models: Paclitaxel-induced rats neuropathy models[1]
Doses: 50 mg/kg Route of Administration: Intraperitoneally injection; on days 0, 1, 2, 4, 7, 9 Experimental Results: Prevented tactile allodynia. Reduced serum neurofilament light chain (NfL) levels. Maintained intraepidermal nerve fiber (IENF) density. In vivo animal studies use Sprague‑Dawley rats for CIPN: paclitaxel (PTX) 5 mg/kg i.p. on days 0,2,4,6,8; Carba1 50 mg/kg i.p. on days ‑2,‑1,0,2,4,6,8. Endpoints: tactile allodynia (von Frey test), serum NfL, IENF density, and DRG histology. For tumor efficacy, female nude mice bearing HeLa or other xenografts receive Carba1 (60 mg/kg i.v. every 2 days for 10 days) with or without PTX. Tumor volume measured by calipers. |
| ADME/Pharmacokinetics |
Detailed PK parameters (t1/2, Cₘₐₓ, AUC, oral bioavailability) are not publicly available. Carba1 is administered via intraperitoneal (50 mg/kg) or intravenous (60 mg/kg) routes in preclinical studies. It is stable as powder at -20 degC for up to 3 years, and in solvent at -80 degC for 1 year. The compound is stable at ambient temperature for several days during ordinary shipping. Solubility: DMSO, may require co‑solvents for in vivo formulations.
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| Toxicity/Toxicokinetics |
Carba1 shows a favorable safety profile in preclinical models. In a rat PTX‑induced neuropathy model, at high doses (50 mg/kg i.p., repeated doses) no detectable toxicity was observed based on blood markers and body weight monitoring. The compound does not promote tumor growth nor inhibit PTX's antitumor efficacy. Minimal intrinsic cytotoxicity: GI₅0 >25 microM in dividing cells. Safety Data Sheets are not publicly available; standard laboratory safety precautions should be followed (gloves, lab coat, eye protection).
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| References | |
| Additional Infomation |
Carba1 is a preclinical research compound discovered by Saxol SAS (formerly Saxol project) and reported in a 2025 preprint (bioRxiv 2025.03.10.642317). Its mechanism of action is dual: (1) microtubule destabilization via colchicine‑site binding to reduce taxane doses; (2) NAMPT activation to enhance NAD+ biosynthesis and neuronal metabolic resilience. It has not entered clinical trials nor been approved by any regulatory authority. A related patent has been filed (European patent 24305705.6). The company plans to begin clinical trials by 2028.
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| Molecular Formula |
C18H15CLN2
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| Molecular Weight |
294.78
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| Exact Mass |
294.092
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| CAS # |
2635394-10-2
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| PubChem CID |
155926995
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
1
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
21
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| Complexity |
381
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=CC(=C(C2=C1NC3=C2C=C(C=C3)Cl)C)N4C=CC=C4
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| InChi Key |
ACQHOGDRJNVGBV-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H15ClN2/c1-11-9-16(21-7-3-4-8-21)12(2)17-14-10-13(19)5-6-15(14)20-18(11)17/h3-10,20H,1-2H3
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| Chemical Name |
6-chloro-1,4-dimethyl-3-pyrrol-1-yl-9H-carbazole
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.3924 mL | 16.9618 mL | 33.9236 mL | |
| 5 mM | 0.6785 mL | 3.3924 mL | 6.7847 mL | |
| 10 mM | 0.3392 mL | 1.6962 mL | 3.3924 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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