| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
| ln Vitro |
Rovalpituzumab tesirine (0.01-10000 pM, 96 h) can effectively bind to mouse DLL3 in KP1 cells (SCLC model) expressing mouse DLL3, exhibiting strong killing effect and exerting cytotoxicity through the internalization of PBD toxin [2].
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| ln Vivo |
In a mouse model of small cell lung cancer (SCLC), Rovalpituzumab tesirine (0.03, 0.1, 0.3 mg/kg, single intraperitoneal injection) inhibited tumor growth in a dose-dependent manner, with the 0.3 mg/kg group achieving complete remission. The anti-tumor effect was more significant when used in combination with anti-PD-1 antibody [2]. In a mouse model of SCLC, Rovalpituzumab tesirine (0.03 mg/kg, intraperitoneal injection every four days) combined with anti-PD-1 antibody promoted the infiltration and activation of CD8+ T cells in the tumor, upregulated the expression of PD-L1 and MHC1, overcame immunosuppression, and activated the DC and STING pathways, thus exerting a synergistic anti-tumor effect [2]. In a mouse model of SCLC, the combined use of Rovalpituzumab tesirine (0.1 mg/kg, single intraperitoneal injection) and anti-PD-1 antibody indicated that CD8+ T cells are key effector cells for therapeutic efficacy [2]. In the SCLC mouse model, Rovalpituzumab tesirine (0.03 mg/kg, once intraperitoneal injection) combined with anti-PD-1 can induce long-term anti-tumor immune memory [2].
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| Animal Protocol |
Animal/Disease Models:B6129SF1/J mice (female, 6-8 weeks old) were injected with KP1 cells (1 × 10⁶ cells) [2]
Doses: 0.03 mg/kg Route of Administration: Intraperitoneal injection, single dose Experimental Results: The results showed that both monotherapy and combination therapy significantly increased the proliferation and activation of CD45⁺ immune cells and CD8⁺ T cells in the tumor. Rp regulates the expression of immune activation-related genes (such as granzyme B, IFNγ, IL-12β) and chemokines (CCL5, CXCL10), and induces the expression of PDL1 and MHC1, demonstrating the rationality of combination therapy with anti-PD-1 antibody. |
| References |
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| Molecular Formula |
C78H108N10O25S
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|---|---|
| Molecular Weight |
148013 (average)
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| CAS # |
1613313-09-9
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| Appearance |
Colorless to light yellow liquid
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| SMILES |
[Rovalpituzumab tesirine]
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| Synonyms |
SC-002
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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: 本产品在运输和储存过程中需避光（避免光照）。 |
| 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.) |
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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