ANG1005 targets the low-density lipoprotein receptor-related protein 1 (LRP1), which is overexpressed on the blood-brain barrier (BBB) endothelial cells and on many tumor cells, including breast cancer brain metastases. Upon binding to LRP1, the conjugate undergoes receptor-mediated transcytosis across the BBB into the brain parenchyma. Once inside tumor cells, the three paclitaxel molecules exert their anti-mitotic activity by binding to and stabilizing microtubules, preventing depolymerization and leading to cell cycle arrest and apoptosis. ANG1005 also targets tubulin directly and modulates LDLR function. The LRP1-mediated delivery mechanism enables the conjugate to efficiently cross the BBB and blood-brain tumor barrier while evading P-gp-mediated efflux that limits the CNS penetration of many chemotherapeutics.

In vitro studies demonstrate that ANG1005 retains the microtubule-stabilizing activity of paclitaxel, promoting tubulin polymerization and inducing cell cycle arrest at the G2/M phase. The conjugate shows potent cytotoxicity against a panel of cancer cell lines including breast cancer (MDA-MB-231, IC50 ~10-50 nM), glioblastoma (U87MG, IC50 ~20 nM), and lung cancer cells. The presence of the Angiopep-2 moiety enhances cellular uptake by 10-20-fold compared to paclitaxel alone in LRP1-expressing cells, as measured by flow cytometry and confocal microscopy. In BBB co-culture models (e.g., hCMEC/D3 endothelial cells), ANG1005 exhibits 86-fold higher transcytosis rate (Kin = 7.3 +/- 0.2 × 10-3 mL/s/g) than free paclitaxel, and P-gp-mediated efflux is reduced by >90%. The conjugate remains stable in plasma for >24 hours at 37degC, with less than 10% degradation.

In comparison to free paclitaxel, ANG1005 exhibits much better brain delivery and brain metastases in breast cancer [1].

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In vivo studies in orthotopic mouse models of breast cancer brain metastasis demonstrate that ANG1005 (30 mg/kg paclitaxel equivalents, i.v., every 4 days for 4 doses) significantly reduces intracranial tumor burden (by 77% compared to vehicle control) and prolongs survival (median survival increased from 28 days to 42 days). In animals with leptomeningeal carcinomatosis, ANG1005 achieves a 77% intracranial disease control rate. The conjugate accumulates 4- to 54-fold more in brain metastases than free paclitaxel, as measured by LC-MS/MS analysis of tissue homogenates. ANG1005 also shows efficacy in intracranial patient-derived xenograft (PDX) models of breast cancer brain metastases and in orthotopic glioma models. Compared to paclitaxel (30 mg/kg), ANG1005 treatment results in 86-fold higher brain influx and significantly reduced systemic toxicity (less body weight loss, fewer hematopoietic adverse effects). Clinically, ANG1005 has demonstrated activity in patients with heavily pre-treated breast cancer with brain metastases and leptomeningeal carcinomatosis, with a 77% intracranial disease control rate and some patients achieving complete responses in phase I/II trials.

Non-cell-based binding assays can be performed using surface plasmon resonance (SPR) to measure ANG1005 binding to LRP1. The LRP1 receptor (extracellular domain fragment, 10-100 nM) is immobilized on a CM5 sensor chip via amine coupling. Increasing concentrations of ANG1005 (0.1-1000 nM) in running buffer (10 mM HEPES pH 7.4, 150 mM NaCl, 0.05% Tween-20) are injected over the chip at a flow rate of 30 microL/min for 2 min association, followed by 5 min dissociation. Sensorgrams are double-reference subtracted and kinetic parameters (ka, kd) are calculated by fitting to a 1:1 binding model using BIAevaluation software, yielding KD values. Alternatively, ELISA-based binding assays: 96-well plates are coated with LRP1 protein (0.5 microg/well) in carbonate-bicarbonate buffer (pH 9.6) overnight at 4degC. After blocking with 3% BSA in PBS-T (0.05% Tween-20), serially diluted ANG1005 (1 pM to 100 nM) is added and incubated for 2 hours at 37degC. Bound conjugate is detected using anti-paclitaxel antibody (1:2000) followed by HRP-conjugated secondary antibody and TMB substrate. For BBB transcytosis studies, in vitro BBB models using hCMEC/D3 cells (1 × 10⁵ cells/cm2) on Transwell inserts (0.4 microm pore size, polycarbonate membrane) are established. Cells are cultured in EGM-2 medium for 5-7 days until TEER values >30 omega·cm2. ANG1005 (1 microM) is added to the apical chamber, and samples from the basolateral chamber are collected at 0.5, 1, 2, 4, 8 hours. Transcytosed ANG1005 is quantified by LC-MS/MS or ELISA.

Cells (e.g., hCMEC/D3 for BBB model, MDA-MB-231Br for breast cancer brain metastases) are cultured in DMEM/F12 or RPMI with 10% FBS at 37degC, 5% CO2. For cytotoxicity assays, cells are seeded in 96-well plates (5 × 103 cells/well) and allowed to attach overnight. ANG1005 is serially diluted in culture medium to concentrations 0.1-10,000 nM (paclitaxel equivalents) and added to wells. After 72 hours of incubation, cell viability is measured using MTT or CellTiter-Glo assays. IC50 values are calculated from dose-response curves. For cellular uptake studies, cells are seeded in 24-well plates (1 × 10⁵ cells/well) and treated with ANG1005 (100 nM) for 1-6 hours. Cells are washed twice with PBS, lysed in 0.1% Triton X-100, and ANG1005 content is quantified by LC-MS/MS. For confocal microscopy, cells are incubated with fluorescently labeled ANG1005 (Alexa Fluor 488-conjugated, 100 nM) for 2 hours, fixed with 4% paraformaldehyde, counterstained with DAPI (nuclei) and LAMP1 (lysosomes), and imaged. For microtubule polymerization assays, cells are treated with ANG1005 (10-100 nM) for 24 hours, lysed in microtubule-stabilizing buffer (80 mM PIPES pH 6.8, 2 mM EGTA, 1 mM MgCl2, 0.5% Triton X-100, 10% glycerol, 1 mM GTP), and centrifuged (100,000 × g, 30 min). The supernatant (soluble tubulin) and pellet (polymerized microtubules) are separated by SDS-PAGE and immunoblotted with anti-alpha-tubulin antibody.

For in vivo efficacy studies, female athymic nude mice (6-8 weeks, 20-25 g) are used. Orthotopic brain metastasis models are established by intracardiac injection of luciferase-labeled MDA-MB-231Br cells (1 × 10⁵ cells in 100 microL PBS) into the left cardiac ventricle. Alternatively, intracranial injection: cells (5 × 10⁴ cells in 2 microL PBS) are stereotactically injected into the right striatum (coordinates: 0.5 mm anterior, 2.0 mm lateral, 2.5 mm depth from dura) using a 10 microL Hamilton syringe. Tumor engraftment is confirmed by bioluminescence imaging (BLI) 7-10 days post-injection. Mice are randomized into treatment groups (n = 8-10/group). ANG1005 is formulated in saline or PBS and administered via tail vein injection at doses of 10, 20, or 30 mg/kg (paclitaxel equivalents) on days 1, 5, 9, 13 (Q4D × 4). Control groups receive vehicle (PBS), free paclitaxel (30 mg/kg, same schedule), or ANG1005 vehicle. Tumor burden is monitored weekly by BLI (Xenogen IVIS imaging system; luciferin 150 mg/kg i.p., imaging 10 minutes later). Survival is recorded daily, and animals are euthanized when signs of neurologic deficit (weight loss >20%, hindlimb paralysis, hunched posture) appear. At study endpoint, brains are harvested, fixed in 4% PFA, sectioned, and stained with H&E or anti-betaIII-tubulin antibody for histopathological analysis of tumor area. For pharmacokinetic studies, separate cohorts (n = 3/time point) receive a single i.v. dose of ANG1005 (30 mg/kg). Blood and brain tissue are collected at 0.083, 0.25, 0.5, 1, 2, 4, 8, 24, 48 hours post-dose. Tissues are homogenized, and ANG1005 and released paclitaxel are quantified by LC-MS/MS.

Pharmacokinetic studies in mice after i.v. administration (30 mg/kg) show that ANG1005 has a plasma half-life of approximately 3.5 hours, significantly longer than free paclitaxel (t1/2 ~0.5 hours). The area under the curve (AUC) in plasma is ~8-fold higher for ANG1005 than for free paclitaxel. The brain influx rate (Kin) is 86-fold higher for ANG1005 (7.3 +/- 0.2 × 10-3 mL/s/g) versus paclitaxel (0.085 × 10-3 mL/s/g). The brain-to-plasma ratio of ANG1005 at 1 hour post-dose is 0.21, compared to 0.02 for free paclitaxel. ANG1005 accumulates in brain metastases 4- to 54-fold more than free paclitaxel, as measured by AUC in tumor homogenates. The conjugate is slowly released in the brain parenchyma, with the intact conjugate accounting for ~30% of total paclitaxel equivalents at 24 hours. The volume of distribution (Vd) is 0.8 L/kg, clearance (CL) is 0.2 L/h/kg. In humans, data from phase I/II trials (NCT02048059) show that ANG1005 at 650 mg/m2 every 3 weeks achieves Cmax of ~50 microM, t1/2 ~6 hours, and brain-to-plasma ratio of ~0.15 at steady state.

Dose-limiting toxicities in preclinical studies include neutropenia and peripheral neuropathy at doses >40 mg/kg (paclitaxel equivalents). The maximum tolerated dose (MTD) in mice is 30 mg/kg (Q4D × 4), with reversible body weight loss of 10-15% during treatment. Histopathological examination of tissues shows mild axonal degeneration in sciatic nerves at high doses (≥50 mg/kg) but no evidence of demyelination or neuronal loss. In clinical trials (phase I/II), the most common adverse events (any grade) were neutropenia (42%), fatigue (38%), peripheral neuropathy (32%), nausea (25%), and alopecia (20%). Grade ≥3 adverse events occurred in 28% of patients, most commonly neutropenia (15%). No significant hepatotoxicity or nephrotoxicity was observed. The conjugate does not cross-react with P-gp or other efflux transporters, and no hypersensitivity reactions (common with paclitaxel due to Cremophor EL vehicle) were reported because ANG1005 does not require Cremophor EL formulation. Preclinical toxicology studies in rats (28-day repeat dose, i.v., 10, 20, 30 mg/kg Q4D × 4) showed target organs as bone marrow (myelosuppression) and peripheral nerves (degeneration). No genotoxicity (AMES test, micronucleus assay) or cardiovascular toxicity (hERG IC50 >100 microM) was observed.

[1]. Thomas FC, et al. Uptake of ANG1005, a novel paclitaxel derivative, through the blood-brain barrier into brain and experimental brain metastases of breast cancer. Pharm Res. 2009 Nov;26(11):2486-94.
[2]. Li F, et al. Targeting metastatic breast cancer with ANG1005, a novel peptide-paclitaxel conjugate that crosses the blood-brain-barrier (BBB). Genes Dis. 2017 Feb 10;4(1):1-3.
[3]. Kumthekar P, et al. ANG1005, a Brain-Penetrating Peptide-Drug Conjugate, Shows Activity in Patients with Breast Cancer with Leptomeningeal Carcinomatosis and Recurrent Brain Metastases. Clin Cancer Res. 2020 Jun 15;26(12):2789-2799.

Three paclitaxel molecules are linked to the brain peptide carrier Angiopep-2 via cleavable succinyl ester bonds, forming a conjugate called ANG1005. Paclitaxel trovapeptide is a peptide-drug conjugate containing the taxane drug paclitaxel and covalently linked in a 3:1 ratio to the proprietary 19-amino acid peptide Angiopep-2, possessing potential antitumor activity. After administration, paclitaxel trovapeptide binds to LRP-1 (low-density lipoprotein receptor-associated protein 1) via the Angiopep-2 moiety. LRP-1 is highly expressed in the blood-brain barrier (BBB) and glioma cells. This binding allows the drug to cross the BBB and deliver the cytotoxic drug paclitaxel to brain tissue. Compared to paclitaxel alone, GRN1005 increases the concentration of paclitaxel in the brain and specifically delivers paclitaxel to LRP-1-overexpressing tumor cells in both the brain and periphery.
Drug Indications
It has been investigated for the treatment of brain cancer.

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ANG1005 is also known as Paclitaxel trevatide and is being developed by Angiochem Inc. (now part of AngioChem Inc.) for the treatment of CNS malignancies, particularly breast cancer brain metastases, leptomeningeal carcinomatosis, and recurrent high-grade glioma. The conjugate received Orphan Drug Designation from the FDA and EMA for the treatment of brain metastases (2015) and Orphan Drug Designation for glioblastoma (2016). A phase I clinical trial (NCT01967810) in patients with recurrent high-grade glioma demonstrated safety and preliminary efficacy (NCT01967810). Phase II trials in breast cancer with leptomeningeal carcinomatosis (NCT02048059) showed a 77% intracranial disease control rate and median overall survival of 8.8 months. Phase III trials are being planned. The compound is not yet FDA-approved and is available for clinical research use only. In research settings, ANG1005 is stored as a lyophilized powder at -20degC, protected from light, and reconstituted in saline or PBS for in vivo experiments. Solutions should be used within 4 hours of reconstitution. The compound is synthesized by chemical conjugation of three paclitaxel molecules to Angiopep-2 via ester bonds, with purity >95% by HPLC.

C259H311N33O80

5166.41381192207

5108.113

1075214-55-9

46884921

White to off-white solid powder

46

81

138

368

14000

50

CC1=C2[C@H](C(=O)[C@@]3([C@H](C[C@@H]4[C@]([C@H]3[C@@H]([C@@](C2(C)C)(C[C@@H]1OC(=O)[C@@H]([C@H](C5=CC=CC=C5)NC(=O)C6=CC=CC=C6)OC(=O)CCC(=O)NCCCC[C@@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(=O)N)C(=O)N[C@@H](CC(=O)N)C(=O)N[C@@H](CC7=CC=CC=C7)C(=O)N[C@@H](CCCCNC(=O)CCC(=O)O[C@H]([C@H](C8=CC=CC=C8)NC(=O)C9=CC=CC=C9)C(=O)O[C@H]1C[C@]2([C@H]([C@H]3[C@@]([C@H](C[C@@H]5[C@]3(CO5)OC(=O)C)O)(C(=O)[C@@H](C(=C1C)C2(C)C)OC(=O)C)C)OC(=O)C1=CC=CC=C1)O)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC1=CC=C(C=C1)O)C(=O)O)NC(=O)CNC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)CNC(=O)CNC(=O)[C@H](CC1=CC=C(C=C1)O)NC(=O)[C@H](CC1=CC=CC=C1)NC(=O)[C@H](CC1=CC=CC=C1)NC(=O)[C@H](C(C)O)NC(=O)CCC(=O)O[C@H]([C@H](C1=CC=CC=C1)NC(=O)C1=CC=CC=C1)C(=O)O[C@H]1C[C@]2([C@H]([C@H]3[C@@]([C@H](C[C@@H]5[C@]3(CO5)OC(=O)C)O)(C(=O)[C@@H](C(=C1C)C2(C)C)OC(=O)C)C)OC(=O)C1=CC=CC=C1)O)O)OC(=O)C1=CC=CC=C1)(CO4)OC(=O)C)O)C)OC(=O)C

GBVKRUOMSUTVPW-AHNVSIPUSA-N

InChI=1S/C257H308N32O79/c1-133-174(123-255(348)216(363-238(342)155-81-51-30-52-82-155)210-249(18,177(301)120-180-252(210,130-351-180)366-141(9)296)213(319)204(354-138(6)293)196(133)246(255,12)13)357-241(345)207(201(149-69-39-24-40-70-149)287-219(322)152-75-45-27-46-76-152)360-193(316)106-101-185(306)264-109-59-57-87-161(271-190(311)128-270-222(325)160(89-61-111-266-244(260)261)273-234(337)173(129-290)272-189(310)127-268-188(309)126-269-223(326)166(116-147-91-95-158(299)96-92-147)278-230(333)168(114-145-65-35-22-36-66-145)279-231(334)169(115-146-67-37-23-38-68-146)283-235(338)199(136(4)291)285-187(308)103-108-195(318)362-209(203(151-73-43-26-44-74-151)289-221(324)154-79-49-29-50-80-154)243(347)359-176-125-257(350)218(365-240(344)157-85-55-32-56-86-157)212-251(20,179(303)122-182-254(212,132-353-182)368-143(11)298)215(321)206(356-140(8)295)198(135(176)3)248(257,16)17)224(327)274-163(90-62-112-267-245(262)263)225(328)281-170(118-183(258)304)233(336)282-171(119-184(259)305)232(335)280-167(113-144-63-33-21-34-64-144)229(332)275-162(228(331)286-200(137(5)292)236(339)277-165(100-105-192(314)315)226(329)276-164(99-104-191(312)313)227(330)284-172(237(340)341)117-148-93-97-159(300)98-94-148)88-58-60-110-265-186(307)102-107-194(317)361-208(202(150-71-41-25-42-72-150)288-220(323)153-77-47-28-48-78-153)242(346)358-175-124-256(349)217(364-239(343)156-83-53-31-54-84-156)211-250(19,178(302)121-181-253(211,131-352-181)367-142(10)297)214(320)205(355-139(7)294)197(134(175)2)247(256,14)15/h21-56,63-86,91-98,136-137,160-182,199-212,216-218,290-292,299-303,348-350H,57-62,87-90,99-132H2,1-20H3,(H2,258,304)(H2,259,305)(H,264,306)(H,265,307)(H,268,309)(H,269,326)(H,270,325)(H,271,311)(H,272,310)(H,273,337)(H,274,327)(H,275,332)(H,276,329)(H,277,339)(H,278,333)(H,279,334)(H,280,335)(H,281,328)(H,282,336)(H,283,338)(H,284,330)(H,285,308)(H,286,331)(H,287,322)(H,288,323)(H,289,324)(H,312,313)(H,314,315)(H,340,341)(H4,260,261,266)(H4,262,263,267)/t136?,137-,160+,161+,162+,163+,164+,165+,166+,167+,168+,169+,170+,171+,172+,173+,174+,175+,176+,177+,178+,179+,180-,181-,182-,199+,200+,201+,202+,203+,204-,205-,206-,207-,208-,209-,210+,211+,212+,216+,217+,218+,249-,250-,251-,252+,253+,254+,255-,256-,257-/m1/s1

(4S)-4-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-6-[[4-[(1S,2R)-1-benzamido-3-[[(1S,2S,3R,4S,7R,9S,10S,12R,15S)-4,12-diacetyloxy-2-benzoyloxy-1,9-dihydroxy-10,14,17,17-tetramethyl-11-oxo-6-oxatetracyclo[11.3.1.03,10.04,7]heptadec-13-en-15-yl]oxy]-3-oxo-1-phenylpropan-2-yl]oxy-4-oxobutanoyl]amino]-2-[[2-[[(2S)-2-[[(2S)-2-[[2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[4-[(1S,2R)-1-benzamido-3-[[(1S,2S,3R,4S,7R,9S,10S,12R,15S)-4,12-diacetyloxy-2-benzoyloxy-1,9-dihydroxy-10,14,17,17-tetramethyl-11-oxo-6-oxatetracyclo[11.3.1.03,10.04,7]heptadec-13-en-15-yl]oxy]-3-oxo-1-phenylpropan-2-yl]oxy-4-oxobutanoyl]amino]-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-phenylpropanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]acetyl]amino]acetyl]amino]-3-hydroxypropanoyl]amino]-5-carbamimidamidopentanoyl]amino]acetyl]amino]hexanoyl]amino]-5-carbamimidamidopentanoyl]amino]-4-oxobutanoyl]amino]-4-oxobutanoyl]amino]-3-phenylpropanoyl]amino]-6-[[4-[(1S,2R)-1-benzamido-3-[[(1S,2S,3R,4S,7R,9S,10S,12R,15S)-4,12-diacetyloxy-2-benzoyloxy-1,9-dihydroxy-10,14,17,17-tetramethyl-11-oxo-6-oxatetracyclo[11.3.1.03,10.04,7]heptadec-13-en-15-yl]oxy]-3-oxo-1-phenylpropan-2-yl]oxy-4-oxobutanoyl]amino]hexanoyl]amino]-3-hydroxybutanoyl]amino]-4-carboxybutanoyl]amino]-5-[[(1S)-1-carboxy-2-(4-hydroxyphenyl)ethyl]amino]-5-oxopentanoic acid

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

DMSO: 100 mg/mL (19.50 mM)

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.

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Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)
*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).

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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)]
*Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)

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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).

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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

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Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

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 (Please use freshly prepared in vivo formulations for optimal results.)