| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
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Purity: =99.11%
| Targets |
Somatostatin receptors (SSTRs), specifically high affinity to SSTR2 subtype[1]
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| ln Vitro |
Receptor affinity studies confirmed 177Lu-DOTATATE exhibits enhanced binding to somatostatin receptors compared to octreotide and Tyr³-octreotide, attributed to the structural modification of the peptide analog (Tyr³-octreotate)[16,17].
No additional in vitro assays (e.g., cell proliferation, apoptosis) were described for 177Lu-DOTATATE in this study.[1] |
| ln Vivo |
Excellent anti-tumor effects of 177Lu-DOTATATE have been observed in rats [1].
In Lewis rats bearing dual CA20948 pancreatic tumors (small: ~0.5 cm²; large: 7–9 cm²), a single intravenous injection of 555 MBq 177Lu-DOTATATE (delivering 60 Gy to large tumors) significantly extended survival vs. controls (P<0.001). 25% of animals survived to 150 days post-treatment (equivalent to ~5 human years), though complete remission was not achieved in large tumors due to clonogenic cell burden. In a rat liver micrometastatic model, 177Lu-DOTATATE demonstrated potent antitumor effects, reducing metastatic burden and improving survival. 177Lu-DOTATATE outperformed 90Y-DOTATOC in small tumors (<10 mm diameter), where its medium-energy β-emissions (0.5 MeV) achieved near-complete energy absorption (97% in 10-mm spheres vs. 66% for 90Y).[1] 177Lu-DOTATATE is clinically used for molecular radiotherapy in metastatic neuroblastoma patients selected by 68Ga-DOTATATE PET positivity. It targets SSTR-2-expressing tumors, with clinical efficacy observed in relapsed/refractory pediatric cases. In a Phase IIa trial, 177Lu-DOTATATE demonstrated therapeutic activity in children with primary refractory or relapsed high-risk neuroblastoma, improving disease control.[2] Demonstrated high radiotherapeutic efficacy in a rat tumor model. [3] Compared [177Lu-DOTA0Tyr3]octreotate with [111In-DTPA0]octreotide in patients, showing potential for 177Lu-labelled peptides in peptide receptor radionuclide therapy (PRRT). [3] |
| Animal Protocol |
Tumor Model: Male Lewis rats (250–300 g) implanted subcutaneously with CA20948 pancreatic tumor cells. Small (~0.5 cm²) and large (7–9 cm²) tumors were established in contralateral flanks[1]
Dosing: Single intravenous injection via dorsal penile vein: - 177Lu-DOTATATE: 555 MBq (specific activity: 37 MBq/μg peptide) or Fractionated dosing (2 injections, 2 weeks apart): 2 × 278 MBq 177Lu-DOTATATE[1] Endpoint Monitoring: Tumor size (caliper measurements), survival, body weight. Euthanasia criteria: tumor >15 cm² or >10% body weight loss.[1] |
| ADME/Pharmacokinetics |
177Lu-DOTATATE rapidly clears from blood due to small peptide size, with sustained retention in SSTR-positive tumors via receptor internalization. Dosimetry assumed uniform spherical tumor distribution; S-values used for absorbed dose calculations.[1]
Optimal labelling conditions for 177Lu were found to be at pH 4–4.5, with reactions completed after 20 minutes at 80°C. [3] Achieved high specific activities, crucial for PRRT. [3] |
| Toxicity/Toxicokinetics |
Clinical data (cited) noted reversible hematological toxicity in humans. Adjacent tissue dose exposure is lower vs. 90Y (e.g., 4–46% of tumor dose for tissues near 131I-like emitters vs. 24–103% for 90Y).[1]
Clinical studies cited note reversible hematological and renal toxicity profiles consistent with PRRT.[2] |
| References |
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| Additional Infomation |
177Lu-DOTATATE combines therapeutic β-emission (0.5 MeV max) and diagnostic γ-emission (113 keV, 6.3%), enabling simultaneous treatment and scintigraphic monitoring[1].
Clinical efficacy: In gastroenteropancreatic neuroendocrine tumor patients, 177Lu-DOTATATE achieved 30% complete/partial remission + 21% minor response rates. Optimal for tumors <10 mm due to short β-particle range (2.1 mm max) and high intratumoral energy absorption (e.g., 93% in 5-mm spheres).[1] 177Lu-DOTATATE is a cornerstone treatment for adult neuroendocrine tumors, improving survival[19]. Its application in pediatric neuroblastoma is emerging. Heterogeneity in SSTR-2 vs. NAT (noradrenaline transporter) expression was observed: 26/42 neuroblastoma patients showed discordant anatomical distribution between 68Ga-DOTATATE (SSTR-2) and 123I-mIBG (NAT) scans. This supports combining 177Lu-DOTATATE with 131I-mIBG to target biologically distinct tumor clones[2]. Optimal patient selection requires 68Ga-DOTATATE PET/CT to confirm SSTR-2 avidity before therapy.[2] Radiolabeling conditions for DOTA-peptides: Optimal labeling with 177Lu occurs at pH 4–4.5 and 80°C for 20 min, achieving >99% incorporation into DOTA-conjugated peptides (e.g., DOTATOC, DOTA-tate). Reaction kinetics are faster for 177Lu than for 90Y or 111In[3]. Maximal achievable specific activity (SA): Theoretical SA is 19 mCi/nmol (Table 1). Experimentally, high SA is achievable even at a molar ratio of DOTA-peptide to 177Lu as low as 1.2:1. Hf4+ (decay product of 177Lu) does not compete for DOTA binding, enabling high SA for ≥2 weeks post-production[3]. Contaminant interference: Zr4+ (90Y decay product) and Hf4+ (177Lu decay product) do not inhibit radiolabeling, whereas Cd2+ (111In decay product) strongly competes (Table 2, Fig. 3)[3]. |
| Molecular Formula |
C65H90N14O19S2.XC2H4O2
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|---|---|
| Molecular Weight |
1435.6225
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| Exact Mass |
1436.61
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| Elemental Analysis |
C, 53.80; H, 6.34; N, 13.11; O, 22.46; S, 4.29
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| CAS # |
177943-89-4
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| Related CAS # |
DOTATATE;177943-88-3
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| PubChem CID |
131634410
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| SequenceShortening |
{DOTA}-{d-Phe}-CY-{d-Trp}-KTCT (Disulfide bridge:Cys2-Cys7)
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
1732.9±65.0 °C at 760 mmHg
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| Flash Point |
1001.8±34.3 °C
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| Vapour Pressure |
0.0±0.3 mmHg at 25°C
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| Index of Refraction |
1.613
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| LogP |
2.7
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| Hydrogen Bond Donor Count |
21
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| Hydrogen Bond Acceptor Count |
34
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| Rotatable Bond Count |
26
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| Heavy Atom Count |
116
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| Complexity |
2740
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| Defined Atom Stereocenter Count |
10
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| SMILES |
NCCCC[C@H](NC([C@H](NC([C@H](CC1=CC=C(O)C=C1)NC([C@H](CS)NC([C@H](NC(CN1CCN(CC(O)=O)CCN(CC(O)=O)CCN(CC(O)=O)CC1)=O)CC1=CC=CC=C1)=O)=O)=O)CC1C2=CC=CC=C2NC=1)=O)C(N[C@@H]([C@@H](C)O)C(N[C@@H](CS)C(N[C@@H]([C@@H](C)O)C(O)=O)=O)=O)=O
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| InChi Key |
YHGBTEQKXYHHPW-TWDDAPNHSA-N
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| InChi Code |
InChI=1S/C65H90N14O19S2.4C2H4O2/c1-38(80)56-64(96)73-51(63(95)75-57(39(2)81)65(97)98)37-100-99-36-50(72-59(91)47(28-40-10-4-3-5-11-40)68-52(83)32-76-20-22-77(33-53(84)85)24-26-79(35-55(88)89)27-25-78(23-21-76)34-54(86)87)62(94)70-48(29-41-15-17-43(82)18-16-41)60(92)71-49(30-42-31-67-45-13-7-6-12-44(42)45)61(93)69-46(58(90)74-56)14-8-9-19-66;4*1-2(3)4/h3-7,10-13,15-18,31,38-39,46-51,56-57,67,80-82H,8-9,14,19-30,32-37,66H2,1-2H3,(H,68,83)(H,69,93)(H,70,94)(H,71,92)(H,72,91)(H,73,96)(H,74,90)(H,75,95)(H,84,85)(H,86,87)(H,88,89)(H,97,98);4*1H3,(H,3,4)/t38-,39-,46+,47-,48+,49-,50+,51+,56+,57+;;;;/m1..../s1
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| Chemical Name |
acetic acid;(2S,3R)-2-[[(4R,7S,10S,13R,16S,19R)-10-(4-aminobutyl)-7-[(1R)-1-hydroxyethyl]-16-[(4-hydroxyphenyl)methyl]-13-(1H-indol-3-ylmethyl)-6,9,12,15,18-pentaoxo-19-[[(2R)-3-phenyl-2-[[2-[4,7,10-tris(carboxymethyl)-1,4,7,10-tetrazacyclododec-1-yl]acetyl]amino]propanoyl]amino]-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]amino]-3-hydroxybutanoic acid
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| Synonyms |
DOTATATE acetate; DOTA-TATE; Oxodotreotide acetate; Dotatate acetate; DOTA-TATE acetate; 99R86Y6V0M; UNII-99R86Y6V0M; L-Threonine, N-((4,7,10-tris(carboxymethyl)-1,4,7,10-tetraazacyclododec-1-yl)acetyl)-D-phenylalanyl-L-cysteinyl-L-tyrosyl-D-tryptophyl-L-lysyl-L-threonyl-L-cysteinyl-, cyclic (2->7)-disulfide, acetate (salt); 177943-89-4; DOTATATE; DOTA TATE; Dotatate; DOTA-octreotate; DOTAoctreotate; DOTA octreotate;
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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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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) |
DMSO: 100 mg/mL
H2O: 8.33 mg/mL |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 11.11 mg/mL (Infinity mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication (<60°C).
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.6966 mL | 3.4828 mL | 6.9656 mL | |
| 5 mM | 0.1393 mL | 0.6966 mL | 1.3931 mL | |
| 10 mM | 0.0697 mL | 0.3483 mL | 0.6966 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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